Quisinostat, also known as JNJ-26481585, is an orally bioavailable, second-generation, hydroxamic acid-based inhibitor of histone deacetylase (HDAC) with potential antineoplastic activity. HDAC inhibitor JNJ-26481585 inhibits HDAC leading to an accumulation of highly acetylated histones, which may result in an induction of chromatin remodeling; inhibition of the transcription of tumor suppressor genes; inhibition of tumor cell division; and the induction of tumor cell apoptosis. HDAC, an enzyme upregulated in many tumor types, deacetylates chromatin histone proteins. Compared to some first generation HDAC inhibitors, JNJ-26481585 may induce superior HSP70 upregulation and bcl-2 downregulation.

Lasofoxifene, also known as CP 336156, is a non-steroidal selective estrogen receptor modulator (SERM) for the prevention and treatment of osteoporosis and for the treatment of vaginal atrophy. In September 2005, Pfizer received a non-approvable letter from the U.S. Food and Drug Administration regarding lasofoxifene (trade name Oporia), a selective estrogen receptor modulator for the prevention of osteoporosis. Lasofoxifene was approved in the EU under the brand name Fablyn by the EMEA in March 2009. Lasofoxifene is a desmethyl dihydro analog of nafoxidine. (source: http://en.wikipedia.org/wiki/Lasofoxifene).

Nemorubicin, also known as PNU152243A, is a doxorubicin derivative that differs significantly from its parent drug in terms of spectrum of antitumor activity, metabolism and toxicity profile. The drug is active on tumors resistant to alkylating agents, topoisomerase II inhibitors and platinum derivatives. It works primarily through topoisomerase I inhibition. Of note, Nemorubicin is active in cells with upregulation of the nucleotide excision repair (NER) pathway, where current therapies fail. Nemorubicin is biotransformed in the liver into cytotoxic metabolites that may further contribute to render this drug highly active against primary liver tumors or liver metastases.

Mifepristone is a synthetic steroid compound used as a pharmaceutical. It is used as an abortifacient in the first two months of pregnancy, and in smaller doses as an emergency contraceptive. During early trials, it was known as RU-486, its designation at the Roussel Uclaf company, which designed the drug. The drug was initially made available in France, and other countries then followed—often amid controversy. It is marketed under tradenames Mifegyne and Mifeprex.

Motexafin lutetium is a texaphyrin, marketed as Antrin by Pharmacyclics Inc. Motexafin lutetium is structurally a pentadentate aromatic metallotexaphyrin with photosensitizing properties. Motexafin lutetium preferentially accumulates in tumor cells due to their increased rates of metabolism and absorbs light, forming an extended high energy conformational state that produces high quantum yields of singlet oxygen, resulting in local cytotoxic effects. M otexafin lutetium is a photosensitiser for use in photodynamic therapy to treat skin conditions and superficial cancers. It has also been tested for use in photoangioplasty (photodynamic treatment of diseased arteries). It is photoactivated by 732 nm light which allows greater depth of penetration.

NOV-002, also known as Glutathione disulfide, GSSG; oxidized glutathione, is a dimer of glutathione with potential chemoprotective and immunomodulating activities. Mimicking endogenous GSSG, glutathione disulfide acts as a competitive substrate for gamma-glutamyl-transpeptidase (GGT), which may result in the S-glutathionylation of proteins, predominantly actin, a redox stress on endoplasmic reticulum (ER), and ER stress-induced apoptosis; S-glutathionylation may be stimulated by reactive oxygen species (ROS) liberated by a glutathione disulfide NOV-002-induced increase in GGT activity.

ONT-093, also known as OC-144-093, is an orally bioavailable P-glycoprotein pump inhibitor, for the potential reversal of multidrug resistance in patients undergoing cancer chemotherapy. ONT-093 could inhibit P-gp and reverse multidrug resistance at nM concentrations with no effect on paclitaxel pharmacokinetics. OC144-093 is the least non-specifically toxic Pgp inhibitor described to date, with an average cytostatic IC50 of >60 microM in 15 cell types. OC144-093 may represent an ideal candidate for use in enhancement of AED blood-brain barrier penetration.

Palifosfamide, also known as ZIO201, is a synthetic mustard compound with potential antineoplastic activity. An active metabolite of ifosfamide covalently linked to the amino acid lysine for stability, palifosfamide irreversibly alkylates and cross-links DNA through GC base pairs, resulting in irreparable 7-atom inter-strand cross-links; inhibition of DNA replication and cell death follow. Unlike ifosfamide, this agent is not metabolized to acrolein or chloroacetaldehyde, metabolites associated with bladder and CNS toxicities. In addition, because palifosfamide does not require activation by aldehyde dehydrogenase, it may overcome the tumor resistance seen with ifosfamide.

Idronoxil, also known as Phenoxodiol, is a synthetic flavonoid derivative. Phenoxodiol activates the mitochondrial caspase system, inhibits X-linked inhibitor of apoptosis (XIAP), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. This agent also inhibits DNA topoisomerase II by stabilizing the cleavable complex, thereby preventing DNA replication and resulting in tumor cell death.

Pelitrexol is a GARFT inhibitor, and is also a water soluble antifolate with anti-proliferative activity. Pelitrexol inhibits activity of glycinamide ribonucleotide formyltransferase (GARFT), the first folate-dependent enzyme of the de novo purine synthesis pathway essential for cell proliferation. Enzyme inhibition reduces the purine nucleotides pool required for DNA replication and RNA transcription. As a result, this agent causes cell cycle arrest in S-phase, and ultimately inhibits tumor cell proliferation.

Picoplatin is a new generation organic platinum analog with an extended spectrum of antineoplastic activity. Designed to overcome platinum drug resistance, picoplatin alkylates DNA, forming both inter- and intra-strand cross-linkages, resulting in inhibition of DNA replication and transcription, and the induction of apoptosis.

Photochlor, also known as HTTP, is a lipophilic, second-generation, chlorin-based photosensitizer. Upon intravenous administration, HPPH selectively accumulates in the cytoplasm of cancer or pre-cancerous cells. When laser light is applied, a photodynamic reaction between HPPH and oxygen occurs, resulting in the production of cytotoxic free radicals and singlet oxygen and free radical-mediated cell death. Compared to the first-generation photosensitizer porfimer sodium, HPPH shows improved pharmacokinetic properties and causes only mild skin photosensitivity which declines rapidly within a few days after administration.

Pixantrone is a synthetic, noncardiotoxic aza-anthracenedione analogue with potential antineoplastic activity. Pixantrone intercalates into DNA and induces topoisomerase II-mediated DNA strand crosslinks, resulting in inhibition of DNA replication and tumor cell cytotoxicity. Pixantrone is a potentially more effective, less cardiotoxic alternative to doxorubicin for patients with aggressive non-Hodgkin lymphoma (aNHL).

PRLX 93936 is a structural analogue of erastin with potential antineoplastic activity. Erastin analogue PRLX 93936 appears to inhibit mitochondrial outer membrane protein VDACs (voltage-dependent anion channels) 2 and 3, resulting in an oxidative, non-apoptotic cell death. Erastin analogue PRLX 93936 exhibits greater lethality in cell lines harboring mutations in the GTPase protein oncogenes HRAS and KRAS or the serine-threonine protein kinase oncogene BRAF than in non-tumorigenic cell lines. VDACs 2 and 3 are up-regulated in a wide variety of tumor cell lines.

Sonolisib, also known as PX-866, is a small-molecule wortmannin analogue inhibitor of the alpha, gamma, and delta isoforms of phosphoinositide 3-kinase (PI3K) with potential antineoplastic activity. PI3K inhibitor PX-866 inhibits the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) and activation of the PI3K/Akt signaling pathway, which may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.

Quinagolide is a selective, D2 receptor agonist (or prolactin-release inhibitor) that is used for the treatment of elevated levels of prolactin. Quinagolide (Norprolac) was approved in European Community, but not in USA as of December, 2011. Quinagolide prevents the production of a chemical called prolactin. Prolactin is involved in many processes within the body, such as milk production after childbirth and altering levels of hormones involved with controlling the menstrual cycle and fertility. Quinagolide is therefore helpful in reducing prolactin levels to reduce milk production for certain medical reasons and to treat some types of infertility, breast problems and menstrual disorders.

Rubitecan is a semisynthetic agent related to camptothecin with potent antitumor and antiviral properties. Rubitecan binds to and inhibits the enzyme topoisomerase I and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells; this agent also prevents repair of reversible single-strand DNA breaks.

SNS-314 is a synthetic small molecule Aurora kinase (AK) inhibitor with potential antineoplastic activity. Aurora kinase inhibitor SNS-314 selectively binds to and inhibits AKs A and B, which may result in the inhibition of cellular division and proliferation in tumor cells that overexpress AKs. AKs are serine-threonine kinases that play essential roles in mitotic checkpoint control during mitosis.

Stannsoporfin ( SnMP), also known as Tin mesoporphyrin, is a porphyrin-Sn(IV) complex, is also a potent heme oxygenase inhibitor, that inhibits HO-1–mediated heme catabolism with potential medicinal application for the treatment of both neonatal jaundice and inherited hyperbilirubinemia syndromes. It was developed to possess unique structural and photophysical properties that make it a particularly potent and bioavailable in vivo inhibitor suitable for clinical use in newborns and studies to date have revealed a very favorable therapeutic profile with no significant adverse side effects.

Talaporfin sodium is a natural chlorophyll-based, and water soluble PDT photosensitizer consisting of chlorin e6, derived from chlorophyll, and L-aspartic acid with photosensitizing activity. After intratumoral activation by light emitting diodes, talaporfin sodium forms an extended high energy conformational state that generates singlet oxygen, which can kill target tissues with minimal side effects through vascular closure and apoptosis. Constant illumination can activate each molecule of talaporfin many times, resulting in a continuous supply of singlet oxygen molecules. Talaporfin kills all tumour cells in the targeted zone, rather than only the minority of cells undergoing rapid division, as in the case of chemotherapy.

Taltobulin, also known as HTI-286 and SPA-110, is a fully synthetic analog of the natural tripeptide hemiasterlin, inhibits tubulin polymerization and circumvents transport-based resistance to taxanes. HTI-286 was a potent inhibitor of proliferation (mean IC50 = 2.5 ?± 2.1 nm in 18 human tumor cell lines) and had substantially less interaction with multidrug resistance protein (P-glycoprotein) than currently used antimicrotubule agents, including paclitaxel, docetaxel, vinorelbine, or vinblastine.

Terameprocol, also known as EM-1421, is a semi-synthetic tetra-methylated derivative of nordihydroguaiaretic acid (NDGA) and transcriptional inhibitor with potential antiviral, antiangiogenic, and antineoplastic activities. Terameprocol competes with the transcription factor Sp1 for specific Sp1 DNA binding domains within gene promoter regions during DNA synthesis. In virally-infected cells, blocking of the Sp1 binding site suppresses Sp1-regulated viral promoter activity and gene expression, thereby inhibiting viral transcription and replication.

Timcodar, also known as VX-853, is a novel multidrug resistance Inhibitor. Timcodar was under clinical trials to treat cancaners and other diseases. Timcodar potentiated the activity of ethidium bromide (EtBr), a model efflux substrate, against three clinically significant gram-positive pathogens: Staphylococcus aureus, Enterococcus faecalis, and Streptococcus pneumoniae. Similar to reserpine, VX-853 directly blocked EtBr efflux in S. aureus. Furthermore, VX-853 was effective in lowering the MICs of several clinically used antibiotics, including fluoroquinolones, suggesting that VX-853 are representatives of a new class of bacterial efflux inhibitors with the potential for use in combination therapy.

Uridine triacetate is a drug used in the treatment of hereditary orotic aciduria and to treat patients following an overdose of chemotherapy drugs 5-fluorouracil or capecitabine, or in patients exhibiting early-onset, severe or life-threatening toxicity affecting the cardiac or central nervous system, and/or early-onset, unusually severe adverse reactions (e.g., gastrointestinal toxicity and/or neutropenia) within 96 hours following the end of 5-fluorouracil or capecitabine administration. Uridine triacetate was granted breakthrough therapy designation by FDA in 2015. Uridine triacetate is a prodrug of uridine.

Vinflunine is a bi-fluorinated derivative of the semi-synthetic vinca alkaloid vinorelbine with antitubulin, antineoplastic, and antiangiogenic activities. Vinflunine inhibits tubulin assembly without any stablization of assembled microtubules at concentrations comparable to those of other vinca alkaloids such as vincristine, vinblastine and vinorelbine; this effect on microtubule dynamics results in cell cycle arrest in mitosis and apoptosis. Compared to other vinca alkaloids, this agent binds weakly to the vinca-binding site, indicating that vinflunine may exhibit reduced neurotoxicity.

Xaliproden, also known as SR57746, is a drug which acts as a 5HT1A agonist. It has neurotrophic and neuroprotective effects in vitro, and has been proposed for use in the treatment of several neurodegenerative conditions including amyotrophic lateral sclerosis and Alzheimer's disease.

Bevonium methylsulfate, also known as CG201, is an antimuscarinic agent.

Eflornithine, also known as Difluoromethylornithine, is a difluoromethylated ornithine compound with antineoplastic activity. Eflornithine irreversibly inhibits ornithine decarboxylase, an enzyme required for polyamine biosynthesis, thereby inhibiting the formation and proliferation of tumor cells. Polyamines are involved in nucleosome oligomerization and DNA conformation, creating a chromatin environment that stimulates neoplastic transformation of cells. This agent has been shown to induce apoptosis in leiomyoma cells.

Apoptone, also known as HE3235, is an orally bioavailable adrenal steroid analogue with potential antineoplastic activity. Androstane steroid HE3235 appears to bind the androgen receptor (AR), down-regulating anti-apoptotic genes, such as Bcl-2, while increasing the expression of pro-apoptotic genes, such as caspases. In vitro and in vivo studies indicate that this agent inhibits androstenediol-dependent LNCaP cell tumor growth. In addition, HE3235 may potentiate chemotherapeutic agents by down-regulating ABCG2, the gene encoding the multi-drug resistant (MDR) protein MDR2.

Methyl-5-aminolevulinate hydrochloride cream is a topical cream formulation containing the hydrochloride salt of methyl-5-aminolevulinate, a lipophilic methyl ester of 5-aminolevulinic acid, with photosensitizer prodrug activity. Upon topical administration, methyl-5-aminolevulinate in the cream is selectively absorbed by tumor cells where it is converted to the photosensitizer protoporphyrin IX (PpIX). Upon photoirradiation, PpIX is activated and transfers energy to oxygen, generating singlet oxygen and superoxide and hydroxyl radicals, which may result in free-radical-mediated DNA damage and cell death.

TH9402 is a dibrominated rhodamine derivative and potent photosensitizer and useful in photodynamic therapy. TH9402 eradicates multiple myeloma (MM) and BC cell lines, while sparing more than 50% of normal pluripotential blood stem cells from healthy volunteers. TH9402 offers an excellent potential as an ex vivo photodynamic purging agent for autologous transplantation in MM and BC treatment.

Methoxyamine is an orally bioavailable small molecule inhibitor with potential adjuvant activity. Methoxyamine covalently binds to apurinic/apyrimidinic (AP) DNA damage sites and inhibits base excision repair (BER), which may result in an increase in DNA strand breaks and apoptosis. This agent may potentiate the anti-tumor activity of alkylating agents. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

GSK1059615 is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. PI3K inhibitor GSK1059615 inhibits PI3K in the PI3K/AKT kinase signaling pathway, which may trigger the translocation of cytosolic Bax to the mitochondrial outer membrane and an increase in mitochondrial membrane permeability, followed by apoptosis. Bax is a member of the proapoptotic Bcl-2 family of proteins. PIK3, an enzyme often overexpressed in cancer cells, plays a crucial role in tumor cell regulation and survival. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Nitroarginine, or Nω-nitro-L-arginine, is a nitro derivative of the amino acid arginine. It is an inhibitor of nitric oxide synthase and hence a vaso-constrictor and coronary constrictor. As such, it finds widespread use as a biochemical tool in the study of nitric oxide and its biological effects. Nitroarginine has been used in research studying coronary constriction, in the presence of midazolam vasodilatation was unaffected by nitroarginine. Nitroarginine is currently in clinical trials for treating patients with advanced solid tumors.

Teriflunomide, aslo known as A77 1726, is the active metabolite of leflunomide. Teriflunomide is an immunomodulatory drug inhibiting pyrimidine de novo synthesis by blocking the enzyme dihydroorotate dehydrogenase. It is uncertain whether this explains its effect on MS lesions. Teriflunomide inhibits rapidly dividing cells, including activated T cells, which are thought to drive the disease process in MS. It has been found that teriflunomide blocks the transcription factor NF-κB. The drug was approved by the FDA on September 13, 2012.

VAL-083 is a bi-functional alkylating agent, with potential antineoplastic activity. Upon administration, VAL-083 crosses the blood brain barrier (BBB) and appears to be selective for tumor cells. This agent alkylates and crosslinks DNA which ultimately leads to a reduction in cancer cell proliferation. In addition, VAL-083 does not show cross-resistance to other conventional chemotherapeutic agents and has a long half-life in the brain.

Pivanex, also known as AN-9, is a histone deacetylase inhibitor analog of butyric acid that causes apoptosis of cancer cells through signaling cellular differentiation. AN-9 exerts a significant anticancer activity in vitro and in vivo.

Nifurtimox is a 5-nitrofuran and is used to treat diseases caused by trypanosomes including Chagas disease and sleeping sickness. It is given by mouth and not by injection. Nifurtimox is now in a Phase II clinical trial for the treatment of pediatric neuroblastoma and medulloblastoma. Nifurtimox decreased cell viability in a concentration-dependent manner. Nifurtimox also suppressed basal and TrkB-mediated Akt phosphorylation, and the cytotoxicity of nifurtimox was attenuated by a tyrosine hydroxylase inhibitor (alpha-methyl-tyrosine). Nifurtimox killed catecholaminergic, but not cholinergic, autonomic neurons in culture. In vivo xenograft models showed inhibition of tumor growth with a histologic decrease in proliferation and increase in apoptosis. These results suggest that nifurtimox induces cell death in neuroblastoma . Therefore, further studies are warranted to develop nifurtimox as a promising new treatment for neuroblastoma.

VRT-043198, the active metabolite of VX-765 (Belnacasan), is a Caspase inhibitor. VRT-043198 exhibits 100- to 10,000-fold selectivity against other caspase-3 and -6 to -9. VRT-043198 inhibited the release of interleukin (IL)-1beta and IL-18, but it had little effect on the release of several other cytokines, including IL-1alpha, tumor necrosis factor-alpha, IL-6 and IL-8.

BMS-214662 is a Farnesyltransferase inhibitor , is also a nonsedating benzodiazepine derivative with potential antineoplastic activity. BMS-214662 inhibits the enzyme farnesyltransferase and the post-translational farnesylation of number of proteins involved in signal transduction, which may result in the inhibition of Ras function and apoptosis in susceptible tumor cells. This agent may reverse the malignant phenotype of H-Ras-transformed cells and has been shown to be active against tumor cells with and without Ras mutations.

Lometrexol is a folate analog antimetabolite with antineoplastic activity. As the 6R diastereomer of 5,10-dideazatetrahydrofolate, lometrexol inhibits glycinamide ribonucleotide formyltransferase (GARFT), the enzyme that catalyzes the first step in the de novo purine biosynthetic pathway, thereby inhibiting DNA synthesis, arresting cells in the S phase of the cell cycle, and inhibiting tumor cell proliferation. The agent has been shown to be active against tumors that are resistant to the folate antagonist methotrexate.

Dilmapimod, also known as SB-681323 and GW-681323 , is p38 MAPK inhibitor. SB-681323 inhibited the p38 MAPK pathway to a greater degree than prednisolone did. SB-681323 inhibited TNF-alpha production. SB-681323 is a potent p38 MAPK inhibitor that potentia

Tiazofurin is a synthetic nucleoside analogue with antineoplastic activity. Tiazofurin (TR) is anabolized intracellularly to an analogue of NAD, tiazole-4-carboxamide adenine dinucleotide (TAD), a potent inhibitor of IMP dehydrogenase (IMPDH); IMPDH is the rate-limiting enzyme for de novo purine synthesis. Inhibition of IMPDH results in reduced levels of guanylates, resulting in the inhibition tumor cell growth in vitro and in vivo.

Timonacic is a cyclic sulfur amino acid derivative with potential antineoplastic and antioxidant activities. Acting on cellular membranes of malignant cells through an unknown mechanism, timonacic may induce malignant cells to revert back to an untransformed state. This agent may also restore contact inhibition, a phenomenon characterized by the paracrine inhibition of mitosis following the formation of a critical cell mass, presumably the result of cell-to-cell signal transfer. Timonacic may also produce antioxidant effects secondary to its release of cysteine and restoration of glutathione concentrations.

TLN-232, also known as CAP-232, is a synthetic cyclic heptapeptide with potential antineoplastic activity. Pyruvate kinase (PK) inhibitor TLN-232 targets pyruvate kinase M2 (M2PK), which may disrupt tumor cell anaerobic glycolysis. M2PK is a dimeric isoform of PK and the predominant PK isoform found in tumor cells.

Trofosfamide is an orally bioavailable oxazaphosphorine prodrug with antineoplastic activity. Trofosfamide (TFF) is metabolized predominantly to the cyclophosphamide analogue ifosfamide (IFO), which is then metabolized by liver cytochrome P450s to the active isophosphoramide mustard (IPM). IPM alkylates DNA to form DNA-DNA cross-links, which may result in inhibition of DNA, RNA and protein synthesis, and tumor cell apoptosis.

Ensartinib, also known as X-396, is an orally available small molecule inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with potential antineoplastic activity. Upon oral administration, X-396 binds to and inhibits ALK kinase, ALK fusion proteins and ALK point mutation variants. Inhibition of ALK leads to the disruption of ALK-mediated signaling and eventually inhibits tumor cell growth in ALK-expressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development.

Pimonidazole, also known as Ro 03-8799 and PD 126675, is a nitroimidazole drug with hypoxic selectivity and radiosensitizing property. Pimonidazole is reduced in hypoxic environments as in tumor cells, thereby it can be used as an hypoxia marker. In hypoxic cells, reduced pimonidazole binds to -SH-containing molecules such as glutathione and proteins, and the resulting complexes accumulated in tissues, thereby sensitizing cells to be more susceptible for radiation treatment.

Etanidazole (SR-2508) is a 2-nitroimidazole drug with radiosensitizing properties. Etanidazole depletes glutathione and inhibits glutathione transferase, thereby enhancing the cytotoxicity of ionizing radiation. This agent may also be useful as an imaging agent for identifying hypoxic, drug-resistant regions of primary tumors or metastases. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Anlotinib, also known as AL3818, is a receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic and anti-angiogenic activities. Upon administration, anlotininib targets multiple RTKs, including vascular endothelial growth factor receptor type 2 (VEGFR2) and type 3 (VEGFR3). This agent may both inhibit angiogenesis and halt tumor cell growth.

Azaserine is a naturally occurring serine derivative diazo compound with antineoplastic properties, Azaserine functions as a purine antagonist and glutamine analogue (glutamine amidotransferase inhibitor) that competitively inhibits pathways in which glutamine is metabolized. An antibiotic and antitumor agent, Azaserine is used in clinical studies as a potential antineoplastic agent.

MI-773 is a new small molecule inhibitor of the MDM2-p53 interaction, binds to MDM2 with high affinity (Ki=0.88 nM) and blocks the p53-MDM2 interaction. MI-773 is an isomer of MI-77301 (SAR405838).

Teroxirone, also known as Triglycidyl Isocyanurate and Tris(2,3-epoxypropyl) Isocyanurate, is a triazene triepoxide with antineoplastic activity. Teroxine alkylates and cross-links DNA, thereby inhibiting DNA replication.

Supinoxin, also known as RX-5902, is orally bioavailable small molecule inhibitor of phosphorylated-p68 RNA helicase (P-p68), with potential anti-proliferative and antineoplastic activity. Upon oral administration, P-p68 inhibitor RX-5902 may both inhibit the activity of the anti-apoptotic B-cell lymphoma 2 (Bcl-2) protein and facilitate the induction of cyclin-dependent kinase inhibitor 1 (p21). This may prevent G2/M cell cycle progression and lead to growth inhibition in tumor cells. P-p68 is overexpressed in various types of solid tumors but absent in normal tissues, and plays a role in tumor progression and metastasis.

Recilisib, also known as ON 01210.Na, is a radioprotectant, which modifys cell cycle distribution patterns in cancer cells subjected to radiation therapy, and it has been identified as a potential candidate for radiation protection studies. It appears that Recilisib radioprotective mechanisms involve prevention of p53-dependent and independent radiation-induced apoptosis.

Carbendazim is a widely used, broad-spectrum benzimidazole fungicide and a metabolite of benomyl. It is also employed as a casting worm control agent in amenity turf situations such as golf greens, tennis courts etc. and in some countries is licensed for that use only. The fungicide is used to control plant diseases in cereals and fruits, including citrus, bananas, strawberries, pineapples, and pomes. It is also controversially used in Queensland, Australia on macadamia plantations. A 4.7% solution of carbendazim hydrochloride, sold as Eertavas, is marketed as a treatment for Dutch elm disease. Studies have found high doses of carbendazim cause infertility and destroy the testicles of laboratory animals. Maximum pesticide residue limits (MRLs) have reduced since discovering its harmful effects. The MRLs for fresh produce in the EU are now between 0.1 and 0.7 mg/kg with the exception of loquat, which is 2 mg/kg. The limits for more commonly consumed citrus and pomme fruits are between 0.1 and 0.2 mg/kg.

Adozelesin, also known as U 73975 or adolezesin, is an experimental antitumor drug of the duocarmycin class. Adozelesin is the first of a class of DNA-sequence-selective alkylating agents, the cyclopropa(c)pyrrolo(3,2-e)indol-4(5H)-ones (CPls), that have been shown to have of potent inhibitory properties of DNA synthesis. It binds to and alkylates DNA, resulting in a reduction of both cellular and simian virus 40 (SV40) DNA replication which ultimately reduces the rate of cancer growth. Phase I and Phase II clinical trials were conducted in 2000s, however, it was found adozelesin had marginal efficacy in the treatment of metastatic breast cancer at the dosage and schedule used.

Ingenol disoxate, also known as LEO43204, is a Novel 4-Isoxazolecarboxylate Ester of Ingenol with Improved Properties for Treatment of Actinic Keratosis and Other Non-Melanoma Skin Cancers. Ingenol is a natural product found in the sap of the plant Euphorbia peplus and an inducer of cell death.

Sacubitrilat, also known as LBQ-657, is endopeptidase inhibitor. Sacubitril is a prodrug that is activated to LBQ657 by de-ethylation via esterases. LBQ657 inhibits the enzyme neprilysin, which is responsible for the degradation of atrial and brain natriuretic peptide, two blood pressure lowering peptides that work mainly by reducing blood volume.

AMG 487 is a potent and selective antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3) with IC50 values of 8nM and 8.2nM for I-IP-10 and I-ITAC, respectively. AMG 487 prevents the chemokines I-IP-10 and I-ITAC from binding to CXCR3. In the cellular assays, AMG 487 inhibits CXCR3-mediated cell migration with IC50 values of 8nM, 15nM and 36nM for I-IP-10, I-ITAC and MIG, respectively.

NBI-74330 is an antagonist of CXC chemokine receptor 3 (CXCR3) with IC50 values of 7nM to18nM. NBI-74330 attenuates atherosclerotic plaque formation in LDL receptor-deficient mice. Chemokine receptor CXCR3 promotes growth of glioma. CXCR3 antagonism exerts a direct anti-glioma effect and this receptor may be a potential therapeutic target for treating human GBM.

Bisantrene, aslo known as CL-216942 and NSC 337766, is topoisomerase II poisons and DNA intercalators. It may be used as model compounds to study P-glycoprotein-mediated multiple drug resistance (MDR1). Bisantrene may be used as a Rac1 inhibitor. Bisantrene intercalates with and disrupts the configuration of DNA, resulting in DNA single-strand breaks, DNA-protein crosslinking, and inhibition of DNA replication. This agent is similar to doxorubicin in activity, but unlike doxorubicin, does not exhibit cardiotoxicity.

Nafoxidine, also known as PNU-0011100 and CP-5600, is a partial estrogen antagonist. Nafoxidine competes with endogenous estrogen for binding to specific estrogen receptors. This agent also inhibits angiogenesis in some tissues by blocking the effects of fibroblast growth factor (FGF) and vascular endothelial growth factor (VEGF); paradoxically, it may enhance angiogenesis in uterine tissue. Nafoxidine also induces oxidative stress, protein kinase C and calcium signaling.

Tetrahydrouridine is a synthetic pyrimidine nucleoside analogue with biomodulating activity. Tetrahydrouridine increases the efficacy of the radiosensitizer cytochlor (5-chloro-2'-deoxycytidine) by inhibiting the enzyme deoxycytidine monophosphate (dCMP) deaminase and preventing the premature deamination of the cytochlor metabolite 5-chloro-2'-deoxycytidine monophosphate (CldCMP) to 5-chloro-2'-deoxyuridine monophosphate (CldUMP); in turn, this increases tumor concentrations of CldUMP which is then further anabolized and incorporated selectively into tumor DNA as CldU (5-chloro-2'-deoxyuridine).

Mafodotin, also known as mc-MMAF and SGD-1269 or Maleimidocaproyl monomethylauristatin F, is a MMAF derivative having a Maleimidocaproyl linker (MC linker), which is ready to conjugate to antibody or other proteins or biopolymers. Mafodotin is a useful a

Diphencyprone, also known as DPCP and Diphenylcyclopropenone, is a topically administered drug intended for treating alopecia areata and alopecia totalis. Topical immunotherapy using diphenylcyclopropenone may also be an effective treatment option for recalcitrant warts. Diphenylcyclopropenone acts as a local irritant, triggering a local sensitization. It triggers an immune response that opposes the action of the autoreactive cells that otherwise cause hair loss.

Carboxyamidotriazole, also known as CAI; RFE-007; NSC-609974; and L-651582, is a novel inhibitor of both cAMP-phosphodiesterases and GMP-phosphodiesterases. Carboxyamidotriazole inhibits oxidative phosphorylation in cancer cells and exerts synergistic anti-cancer effect with glycolysis inhibition. Carboxyamidotriazole ameliorates experimental colitis by inhibition of cytokine production, nuclear factor-κB activation, and colonic fibrosis.

Onalespib lactate, also known as ATI-13387A, is a second-generation, potent and selective HSP90 Inhibitor. Onalespib Blocks mRNA Splicing of Androgen Receptor Variant 7 in Prostate Cancer Cells. Inhibition of HSP90 by AT13387 delays the emergence of resistance to BRAF inhibitors and overcomes resistance to dual BRAF and MEK inhibition in melanoma models. AT13387 induces senescence in EBV-positive nasopharyngeal carcinoma cells and suppresses tumor formation. AT13387, displays a long duration of action in vitro and in vivo in non-small cell lung cancer.

Tiomolibdate diammonium, also known as Ammonium tetrathiomolybdate, is a SOD1 inhibitor with potential antiangiogenic and antitumor activities. ammonium Tiomolibdate diammonium has been found to deplete systemic copper reserves through an unknown mechanism. This agent has been shown to inhibit the activities of cuproenzymes, including superoxide dismutase 1 (SOD1) and cytochrome c oxidase (COX), which may contribute to its antiangiogenic and antitumor effects.

GLL398 is an Oral Selective Estrogen Receptor Downregulator. GLL398 strongly binds to ERα in a fluorescence resonance energy transfer binding assay (IC50 =1.14 nM) and potently degrades ERα in MCF-7 breast cancer cells (IC50 = 0.21 μM). Most importantly, the introduction of the boronic acid group confers superior oral bioavailability of GLL398 (AUC = 36.9 μg·h/mL) in rats as compared to GW7604 (AUC = 3.35 μg·h/mL). The strikingly favorable pharmacokinetic property of GLL398 makes it a promising oral SERD suitable for clinical evaluation.

Orteronel (racemic) is a mixture of S-Orteronel and R-Orteronel isomers. Orteronel, aslo known as TAK-700, is an orally bioavailable non-steroidal androgen synthesis inhibitor of steroid 17alpha-monooxygenase (17,20 lyase) with potential antiandrogen activity. TAK-700 binds to and inhibits the steroid 17alpha-monooxygenase in both the testes and adrenal glands, thereby inhibiting androgen production. This may decrease androgen-dependent growth signaling and may inhibit cell proliferation of androgen-dependent tumor cells.

Rolapitant, also known as SCH-619734, is an orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity. Upon oral administration, rolapitant competitively binds to and blocks the activity of the NK1-receptor in the central nervous system, thereby inhibiting the binding of the endogenous ligand, substance P (SP). This may prevent both SP-induced emesis and chemotherapy-induced nausea and vomiting (CINV).

Prexasertib, also known as LY2606368, is a potent and selective Chk1/Chk2 inhibitor. Prexasertib increases the effectiveness of conventional therapy in B-/T- cell progenitor acute lymphoblastic leukemia. LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms. Treatment of cells with LY2606368 results in the rapid appearance of TUNEL and pH2AX-positive double-stranded DNA breaks in the S-phase cell population.

Ipatasertib, also known as GDC0068, is an orally active, potent and selective Akt inhibitor. GDC-0068 blocked Akt signaling both in cultured human cancer cell lines and in tumor xenograft models. Inhibition of Akt activity by GDC-0068 resulted in blockade of cell-cycle progression and reduced viability of cancer cell lines. Markers of Akt activation, including high-basal phospho-Akt levels, PTEN loss, and PIK3CA kinase domain mutations, correlate with sensitivity to GDC-0068. In multiple tumor xenograft models, oral administration of GDC-0068 resulted in antitumor activity ranging from tumor growth delay to regression.

Ulixertinib, also known as BVD-523 and VRT752271, is an inhibitors of ERK protein kinase. Downmodulation of ERK protein kinase activity inhibits VEGF secretion by human myeloma cells and myeloma-induced angiogenesis. Upon oral administration, BVD-523 inhibits both ERK 1 and 2, thereby preventing the activation of ERK-mediated signal transduction pathways. This results in the inhibition of ERK-dependent tumor cell proliferation and survival. The mitogen-activated protein kinase (MAPK)/ERK pathway is often upregulated in a variety of tumor cell types and plays a key role in tumor cell proliferation, differentiation and survival.

GGTI-298 is a potent geranylgeranyltransferase-I (GGTase-I) inhibitor with potential antitumor actrivity. GGTI-298 disrupts MAP kinase activation and G(1)-S transition in Ki-Ras-overexpressing transformed adrenocortical cells. GGTI-298 induces hypophosphorylation of retinoblastoma and partner switching of cyclin-dependent kinase inhibitors. A potential mechanism for GGTI-298 antitumor activity. GGTI-298 arrests human tumor cells in G0/G1 and induces p21(WAF1/CIP1/SDI1) in a p53-independent manner. GGTI-298 induces G0-G1 block and apoptosis whereas FTI-277 causes G2-M enrichment in A549 cells.

CB-1158-analog, also known as Numidargistat-analog and INCB01158-analog, is a potent and orally active arginase inhibitor with IC50=89 nM) . CB-1158 blocked myeloid cell-mediated suppression of T cell proliferation in vitro and reduced tumor growth in multiple mouse models of cancer, as a single agent and in combination with checkpoint blockade, adoptive T cell therapy, adoptive NK cell therapy, and the chemotherapy agent gemcitabine. CB-1158 increased tumor-infiltrating CD8+ T cells and NK cells, inflammatory cytokines, and expression of interferon-inducible genes. CB-1158 may be potentially useful in renal cell cancer, breast cancer, non-small cell lung cancer, acute myeloid leukemia, and other tumor types where arginase-secreting MDSCs are known to play an immunosuppressive role. (see ADDITIONAL INFORMATION in this web page for CB-1158 structure confusion).

JPH203, also known as KYT-0353, is a potent and selective LAT1 selective ( L-type amino acid transporter 1) inhibitor. JPH203 can very potently inhibit l-leucine uptake. JPH203 inhibits YD-38 cell growth. JPH203 up-regulated the population of apoptotic Y

Givinostat or gavinostat, aslo known as ITF2357, is a potent and orally active histone deacetylase inhibitor with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities. It is a hydroxamate used in the form of its hydrochloride. Inhibition of HDAC activity by ITF2357 ameliorates joint inflammation and prevents cartilage and bone destruction in experimental arthritis.ITF2357 reduces cytokines and protects islet β cells in vivo and in vitro. ITF2357 decreases surface CXCR4 and CCR5 expression on CD4(+) T-cells and monocytes and is superior to valproic acid for latent HIV-1 expression in vitro.

Maytansinoid DM4, a chemical derivative of maytansine, is a potent and selective cytotoxic agent with promising anticancer properties. Anticancer properties of maytansinoids have been attributed to their ability to disrupt microtubule function. Maytansin

Avadomide, also known as CC-122, is an orally available pleiotropic pathway modulator with potential antineoplastic activity. CC-122 mimics an interferon response and has antitumor activity in DLBCL CC-122 binds Cereblon (CRBN) and promotes degradation of Aiolos and Ikaros in diffuse large B-cell lymphoma (DLBCL) and T cells in vitro, in vivo, and in patients, resulting in both cell autonomous as well as immunostimulatory effects.

ONC206 is a chemical analogue of ONC201. ONC206 is a benzyl-flurobenzyl imipridone that has highly potent activity in preclinical models of difficult-to-treat neuroendocrine tumors and sarcomas. ONC206 acts as a selective antagonist of DRD2 at nanomolar concentrations and has broad-spectrum anti-tumor activity. ONC206 may address tumor types where the properties of ONC201 do not permit for complete therapeutic engagement in vivo.

Deltarasin is a high affinity PDEδ-KRAS interaction inhibitor. Deltarasin can inhibit KRAS-PDEδ interactions by binding to a hydrophobic pocket on PDEδ, resulting in the impairment of cell growth, KRAS activity, and RAS/RAF signaling in human pancreatic ductal adenocarcinoma cell lines. The anti-cancer cell activity of deltarasin can be enhanced by simultaneously blocking "tumor protective" autophagy, but inhibited if combined with an anti-oxidant.

Flumatinib, also known as HH-GV-678 , is a selective inhibitor of BCR-ABL/PDGFR/KIT. Flumatinib is currently in Phase I and II clinical trials in China for the treatment of chronic myelogenous leukemia (CML). Flumatinib effectively overcomes drug resistance of certain KIT mutants. Flumatinib mesylate can reduce the expression of C-MYC, HIF-1 α and VEGF in U266 cell line in a time- and dose-dependent manners.

ATN-161 is a small peptide antagonist of integrin alpha5beta1 with potential antineoplastic activity. ATN-161 selectively binds to and blocks the receptor for integrin alpha5beta1, thereby preventing integrin alpha5beta1 binding. This receptor blockade may result in inhibition of endothelial cell-cell interactions, endothelial cell-matrix interactions, angiogenesis, and tumor progression. Integrin alpha5beta1 is expressed on endothelial cells and plays a crucial role in endothelial cell adhesion and migration. Note: The Catalog number of ATN-161 TFA salt was changed from 200350B to 206976.

Filanesib, also known as ARRY-520, is a synthetic, small molecule targeting the kinesin spindle protein (KSP) with potential antineoplastic activity. KSP inhibitor ARRY-520 specifically inhibits KSP (kinesin-5 or Eg5), resulting in activation of the spindle assembly checkpoint, induction of cell cycle arrest during the mitotic phase, and consequently cell death in tumor cells that are actively dividing. Because KSP is not involved in postmitotic processes, such as neuronal transport, this agent does not cause the peripheral neuropathy that is often associated with tubulin-targeting agents.

ONC-201, also known as TIC10 and imipridone, is a potent, orally active, and stable small molecule that transcriptionally induces TRAIL in a p53-independent manner and crosses the blood-brain barrier. TIC10 induces a sustained up-regulation of TRAIL in tumors and normal cells that may contribute to the demonstrable antitumor activity of TIC10. TIC10 inactivates kinases Akt and extracellular signal-regulated kinase (ERK), leading to the translocation of Foxo3a into the nucleus, where it binds to the TRAIL promoter to up-regulate gene transcription. TIC10 is an efficacious antitumor therapeutic agent that acts on tumor cells and their microenvironment to enhance the concentrations of the endogenous tumor suppressor TRAIL.

Miransertib, also known as ARQ 092, is an oral activie, potent and selective AKT inhibitor with IC50 values: 5.0 nM (AKT1); 4.5 nM (AKT2); 16 nM (AKT3). ARQ 092 binds to and inhibits the activity of AKT in a non-ATP competitive manner, which may result in the inhibition of the PI3K/AKT signaling pathway. This may lead to the reduction in tumor cell proliferation and the induction of tumor cell apoptosis. ARQ-092 demonstrated high enzymatic potency against AKT1, AKT2, and AKT3, as well as potent cellular inhibition of AKT activation and the phosphorylation of the downstream target PRAS40. ARQ-092 also served as a potent inhibitor of the AKT1-E17K mutant protein and inhibited tumor growth in a human xenograft mouse model of endometrial adenocarcinoma.

MRX-2843, also known as UNC2371, is a potent and orally active MERTK and FLT3 inhibitor. MRX-2843 overcomes resistance-conferring FLT3 mutations in acute myeloid leukemia. MRX-2843 in combination with an irreversible EGFR TKI as a novel strategy for treatment of patients with wtEGFR NSCLC. MRX-2843 treatment induces apoptosis and inhibits colony formation in AML cell lines and primary patient samples expressing MERTK and/or FLT3-ITD, with a wide therapeutic window compared with that of normal human cord blood cells.

Pexidartinib hydrochloride (PLX-3397 hydrochloride) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib hydrochloride exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib hydrochloride induces cell apoptosis and has anti-cancer activity.

CCS-1477 is a potent and selective p300/CBP bromodomain inhibitor, is targeted & differentiated from BET inhibitors in prostate cancer cell lines in vitro. Combination of CCS1477 & JQ1 resulted in a highly synergistic inhibitory effect on proliferation in normal 22Rv1 cells. Global gene expression analysis revealed significantly fewer altered genes after CCS1477 (27 up, 119 down) compared to JQ1 (196 up, 655 down).

Methylprednisolone acetate, also known as DEPO-MEDROL, is an anti-inflammatory glucocorticoid for intramuscular, intra-articular, soft tissue or intralesional injection. It is available in three strengths: 20 mg/mL; 40 mg/mL; 80 mg/mL.

Tipranavir is a nonpeptidic protease inhibitor. Tipranavir has the ability to inhibit the replication of viruses that are resistant to other protease inhibitors and it recommended for patients who are resistant to other treatments. Resistance to tipranavir itself seems to require multiple mutations. Tipranavir was approved by the Food and Drug Administration (FDA) on June 22, 2005, and was approved for pediatric use on June 24, 2008. Like lopinavir and atazanavir, it is very potent and is effective in salvage therapy for patients with some drug resistance.

Demecarium is a parasympathomimetic that acts as an acetylcholinesterase inhibitor. It is one of several topical (applied directly to the affected area) medications used to reduce elevated intraocular pressure (IOP) associated with primary glaucoma in cats, dogs, and other animals. a cholinesterase inhibitor with sustained activity. It acts mainly on true (erythrocyte) cholinesterase. Application of HUMORSOL (demecarium) to the eye produces intense miosis and ciliary muscle contraction due to inhibition of cholinesterase, allowing acetylcholine to accumulate at sites of cholinergic transmission. These effects are accompanied by increased capillary permeability of the ciliary body and iris, increased permeability of the blood-aqueous barrier, and vasodilation. Myopia may be induced or, if present, may be augmented by the increased refractive power of the lens that results from the accommodative effect of the drug. HUMORSOL (demecarium) indirectly produces some of the muscarinic and nicotinic effects of acetylcholine as quantities of the latter accumulate.

Desmopressin acetate is a synthetic replacement for vasopressin, the hormone that reduces urine production. It may be taken nasally, intravenously, or as a tablet. Doctors prescribe Desmopressin most frequently for treatment of diabetes insipidus or nocturnal enuresis. Desmopressin (1-desamino-8-D-arginine vasopressin) is a modified form of the normal human hormone arginine vasopressin, a peptide containing nine amino acids. Medical use of Desmopressin acetate includes: (a) bed wetting; (b) nighttime urination; (c) clotting disorders; (d) diabetes insipidus.

Tasimelteon (trade name Hetlioz) is a drug approved by the FDA solely for the treatment of non-24-hour sleep?–wake disorder (often designated as N24HSWD) in totally blind adults. It is a selective agonist for the melatonin receptors MT1 and MT2 in the suprachiasmatic nucleus of the brain, similar to other members of the melatonin receptor agonist class of which ramelteon (2005) and agomelatine (2009) were the first approved.

Deferiprone is a drug that chelates iron and is used to treat thalassaemia major. In 1994 was first approved for use in treating thalassaemia major in 1994 and had been licensed for use in Europe and Asia for many years while awaiting approval in Canada and the United States. On October 14, 2011, it was approved for use in the US under the FDA?’s accelerated approval program.

Gabapentin enacarbil is a prodrug for the anticonvulsant and analgesic drug gabapentin. It was designed for increased oral bioavailability over gabapentin, and human trials showed it to produce extended release of gabapentin with almost twice the overall bioavailability, especially when taken with a fatty meal. Gabapentin enacarbil has passed human clinical trials for the treatment of restless legs syndrome, and initial results have shown it to be well tolerated and reasonably effective. (Source: http://en.wikipedia.org/wiki/Gabapentin_enacarbil).

Estradiol valerate is a synthetic ester, specifically the 17-pentanoyl ester, of the natural estrogen, 17β-estradiol. It was introduced in the 1950s, and along with estradiol benzoate and estradiol cypionate, has since become one of the most widely used esters of estradiol. (Source: http://en.wikipedia.org/wiki/Estradiol_valerate).

Icatibant is a peptidomimetic drug consisting of ten amino acids, which is a selective and specific antagonist of bradykinin B2 receptors. It has been approved by the European Commission for the symptomatic treatment of acute attacks of hereditary angioedema (HAE) in adults with C1-esterase-inhibitor deficiency.

Simeprevir, also known as TMC43, is a drug for the treatment and cure of hepatitis C. In the United States, simeprevir is approved by the Food and Drug Administration for use in combination with peginterferon-alfa and ribavirin for hepatitis C and hepatitis B. Simeprevir has been approved in Japan for the treatment of chronic hepatitis C infection, genotype 1.

Levomilnacipran (brand name Fetzima) is an antidepressant approved for the treatment of major depressive disorder in the United States. It was developed by Forest Laboratories and Pierre Fabre Group, and was approved by the Food and Drug Administration in July 2013. Levomilnacipran is the levo- enantiomer of milnacipran, and has similar effects and pharmacology, acting as a serotonin-norepinephrine reuptake inhibitor (SNRI). (Source: http://en.wikipedia.org/wiki/Levomilnacipran)

Tazobactam inhibits the action of bacterial β-lactamases, especially those belonging to the SHV-1 and TEM groups. It is commonly used as its sodium salt, tazobactam sodium. Tazobactam is combined with the extended spectrum β-lactam antibiotic piperacillin in the drug piperacillin/tazobactam, one of the preferred antibiotic treatments for nosocomial pneumonia caused by Pseudomonas aeruginosa.[medical citation needed] Tazobactam broadens the spectrum of piperacillin by making it effective against organisms that express β-lactamase and would normally degrade piperacillin. Tazobactam is derived from the penicillin nucleus and is a penicillinic acid sulfone.

Peramivir, also known as BCX1812 and RWJ 270201, is an antiviral drug for the treatment of influenza. Peramivir is a neuraminidase inhibitor, acting as a transition-state analogue inhibitor of influenza neuraminidase and thereby preventing new viruses from emerging from infected cells. Peramivir was approved to treat influenza infection in adults. (http://en.wikipedia.org/wiki/Peramivir).

Tenofovir alafenamide, also known as TAF and GS-7340, is a nucleotide reverse transcriptase inhibitor (NRTIs) and a novel prodrug of tenofovir. By blocking reverse transcriptase, TAF prevent HIV from multiplying and can reduce the amount of HIV in the body. Tenofovir alafenamide is a prodrug, which means that it is an inactive drug. In the body, tenofovir alafenamide is converted to tenofovir diphosphate (TFV-DP). Tenofovir alafenamide fumarate was approved in November 2015 for treatment of HIV-1.

Fluorogestone Acetate (also known as Flurogestone Acetate, Flugestone Acetate, Fluorogesterone Acetate) was first synthesised by G. D. Searle and Company in 1959. The chemical, which has progestogen activity, was identified as SC-9880. Fluorogestone acetate showed a high potency with short duration of activity and performed physiologically similar to progesterone. FGA was approximately 20 ?– 25 times more potent than progesterone. Flurogestone acetate was shown to be readily absorbed from impregnated sponges. A 30mg impregnated sponge was effective in blocking ovulation and oestrus, once the sponge was removed impregnated ewes showed visible oestrus, and if inseminated 2 to 4 days after sponge removal showed high conception rates. (Source: http://pharmplex.com.au/Technical/fluorogestone_acetate_sheep_goat.htm).

Flumetasone, also known as RS 2177, is a corticosteroid for topical use. It is available in combination with clioquinol, under the trade name Locacorten-Vioform (in some countries Locorten-Vioform), for the treatment of otitis externa and otomycosis.

Ganciclovir (INN) is an antiviral medication used to treat or prevent cytomegalovirus (CMV) infections. Ganciclovir is a synthetic analogue of 2′-deoxy-guanosine. It is first phosphorylated to ganciclovir monophosphate by a viral kinase encoded by the cytomegalovirus (CMV) gene UL97 during infection. Subsequently, cellular kinases catalyze the formation of ganciclovir diphosphate and ganciclovir triphosphate, which is present in 10-fold greater concentrations in CMV or herpes simplex virus (HSV)-infected cells than uninfected cells. A prodrug form with improved oral bioavailability (valganciclovir) has also been developed.

Estriol (also oestriol) is one of the three main estrogens produced by the human body. In pregnant women with multiple sclerosis (MS), estriol reduces the disease's symptoms noticeably, according to researchers at UCLA's Geffen Medical School. Estriol can be a weak or strong estrogen depending on if it is given acutely or chronically when given to immature animals, but is an antagonist when given in combination with estradiol. Estriol may play a role in the development of breast cancer, but based on in vitro research does appear to act as an antagonist to the G-protein coupled estrogen receptor. Though estriol is used as part of the primarily North American phenomenon of bioidentical hormone replacement therapy, it is not approved for use by the FDA or Health Canada. (Source: http://en.wikipedia.org/wiki/Estriol).

Pergolide (Permax, Pergotoliderived) is an ergoline-based dopamine receptor agonist used in some countries for the treatment of Parkinson's disease. Parkinson's disease is associated with low levels of the neurotransmitter dopamine in the brain. Pergolide has some of the same effects as dopamine in the body. In 2007, pergolide was withdrawn from the U.S. market after several published studies revealed a link between the drug and increased rates of valvular dysfunction. (Source: http://en.wikipedia.org/wiki/Pergolide )

Bethanechol chloride, a cholinergic agent, is a synthetic esler which is structurally and pharmacologically related to acetylcholine. It is designated chemically as Z-[(aminocarbony) oxy]-N, N, (V-trimethyl-1-propanaminium chloride. Its molecular formula is C7H17CIN202. It is a white, hygroscopic crystalline powder having a slight amine-like odor, freely soluble in water, and has a molecular weight of 196.68. Each tablet for oral administration contains 5 mg, 10 mg, 25 mg or 50 mg bethanechol chloride, USP Tablets also contain the following inactive ingredients: colloidal silicon dioxide, lactose monohydrate, magnesium stearate, microcrystalline cellulose, sodium starch glycolate, (25 mg and 50 mg) D&C~ Yellow # 10 Lake and FD&C Yellow # 6 Lake.

Betamethasone dipropionate is a glucocorticoid steroid with anti-inflammatory and immunosuppressive abilities. It is applied as a topical cream, ointment, lotion or gel (Diprolene) to treat itching and other minor skin conditions such as eczema. Brand names include Alphatrex, Beta-Val, Diprolene, Diprolene AF, Diprosone, and Luxiq. Minor side-effects include dry skin and mild temporary stinging when applied.

Cyproterone acetate is an antiandrogen, i.e. it suppresses the actions of testosterone (and its metabolite dihydrotestosterone) on tissues. It acts by blocking androgen receptors which prevents androgens from binding to them and suppresses luteinizing hormone (which in turn reduces testosterone levels). Its main indications are prostate cancer, benign prostatic hyperplasia, priapism, hypersexuality and other conditions in which androgen action maintains the disease process. Due to its anti-androgen effect, it can also be used to treat hirsutism, and is a common component in hormone therapy for male-to-female transsexual people.

Deflazacort is a glucocorticoid used as an anti-inflammatory and immunosuppressant. It is sold in the United Kingdom by Shire under the trade name Calcort. in Brazil as Cortax, Decortil, and Deflanil, and in Honduras as Flezacor. It is not available in the United States. Deflazacort is a prodrug. Its potency is around 70?–90% that of prednisone.

Bucillamine is an antirheumatic agent developed from tiopronin. It is mainly used in Japan and Korea. Activity is mediated by the two thiol groups that the molecule contains. Research done in USA showed positive transplant preservation properties.

Mitoquinone mesylate, also known as MitoQ or MitoQ10; is a mitochondria-targeted antioxidant designed to accumulate within mitochondria in vivo in order to protect against oxidative damage. MitoQ comprises a positively charged lipophilic cation that drives its extensive accumulation within the negatively charged mitochondria inside cells. The active antioxidant component of MitoQ is ubiquinone, which is identical to the active antioxidant in Coenzyme Q10. It is this approximately thousand-fold greater concentration of MitoQ within mitochondria that makes it more effective at preventing mitochondrial oxidative damage when compared to untargeted antioxidants such as Coenzyme Q10. NOTE: For the convenience of use, this product is supplied as 200mg /mL solution in ethanol-water (1:1, v/v) solution since pure MitoQ10 is a tar-like or waxy semi-solid and very hard to transfer between containers.

Ebastine, is a H1 antihistamine with low potential for causing drowsiness. It does not penetrate the blood–brain barrier to a significant amount and thus combines an effective block of the H1 receptor in peripheral tissue with a low incidence of central side effects, i.e. seldom causing sedation or drowsiness. After oral administration, ebastine undergoes extensive first-pass metabolism by hepatic cytochrome P450 3A4 into its active carboxylic acid metabolite, carebastine. This conversion is practically complete. Ebastine is a second-generation H1 receptor antagonist that is indicated mainly for allergic rhinitis and chronic idiopathic urticaria.

Acenocoumarol is a coumarin that is used as an anticoagulant. Its actions and uses are similar to those of Warfarin. As a vitamin K antagonist, acenocoumarol inhibits vitamin K epoxide reductase, thereby inhibiting the reduction of vitamin K and the availability of vitamin KH2. This prevents gamma carboxylation of glutamic acid residues near the N-terminals of the vitamin K-dependent clotting factors, including factor II, VII, IX, and X and anticoagulant proteins C and S. This prevents their activity, preventing thrombin formation.

Acetohexamide is a sulfonylurea derivative. Acetohexamide is a hyopglycemic agent with moderate uricosuric activity. Acetohexamide is a first generation medication used in the treatment of diabetes metilus type 2.

Acyclovir monophosphate is the monophosphate ester of Acyclovir. Acyclovir is an antiviral agent with activity against herpes simplex virus types 1 and 2 (HSV-1 and HSV-2) and varicella zoster virus. Acyclovir is converted by a herpesvirus enzyme into acyclovir triphosphate that inhibits the synthesis of deoxyribonucleic acid (DNA) molecules in the virally infected cells, thereby inhibiting viral replication. It induces apoptosis in cells transfected with HSV-TK (suicidal gene therapy).

Adinazolam (brand name: Deracyn) is a benzodiazepine derivative, more specifically, a triazolobenzodiazepine (TBZD). It possesses anxiolytic, anticonvulsant, sedative, and antidepressant properties. Adinazolam was developed by Dr. Jackson B. Hester, who was seeking to enhance the antidepressant properties of alprazolam, which he also developed. Adinazolam was never FDA approved and was never available to the public.

Alclometasone is synthetic glucocorticoid steroid for topical use in dermatology as anti-inflammatory, antipruritic, antiallergic, antiproliferative and vasoconstrictive agent. The prodrug alclometasone dipropionate is marketed as Aclovate by GlaxoSmithKline.

Alfuzosin HCl is a pharmaceutical drug of the alpha-1 blocker class. As an antagonist of the alpha-1 adrenergic receptor, it works by relaxing the muscles in the prostate and bladder neck, making it easier to urinate. It is thus used to treat benign prostatic hyperplasia (BPH). Alfuzosin is marketed in the United States by Sanofi Aventis under the brand name Uroxatral and elsewhere under the tradename Xat or Xatral, and in Egypt under name of Prostetrol. Alfuzosin was approved by the FDA for treatment of BPH in June 2003.

Almitrine Dimesylate (marketed as Duxil by Servier) is a diphenylmethylpiperazine derivative classified as a respiratory stimulant by the ATC. It enhances respiration by acting as an agonist of peripheral chemoreceptors located on the carotid bodies. The drug increases arterial oxygen tension while decreasing arterial carbon dioxide tension in patients with chronic obstructive pulmonary disease. It may also prove useful in the treatment of nocturnal oxygen desaturation without impairing the quality of sleep.

Alprenolol HCl, or alfeprol, alpheprol, and alprenololum (Gubernal, Regletin, Yobir, Apllobal, Aptine, Aptol Duriles), is a non-selective beta blocker as well as 5-HT1A receptor antagonist, used in the treatment of angina pectoris. It is no longer marketed by AstraZeneca, but may still be available from other pharmaceutical companies or generically.

Amantadine is a drug that has U.S. Food and Drug Administration approval for use both as an antiviral and an anti-parkinsonian drug. Amantadine is a weak antagonist of the NMDA-type glutamate receptor, increases dopamine release, and blocks dopamine reuptake. Amantadine probably does not inhibit MAO enzyme. Moreover, the mechanism of its antiparkinsonian effect is poorly understood.[citation needed] The drug has many effects in the brain, including release of dopamine and norepinephrine from nerve endings. It appears to be a weak NMDA receptor antagonist as well as an anticholinergic, specifically a nicotinic alpha-7 antagonist like the similar pharmaceutical memantine.

Amcinonide (trade name Cyclocort) is a topical glucocorticoid used to treat itching, redness and swelling associated with several dermatologic conditions such as atopic dermatitis and allergic contact dermatitis. Amcinonide is a synthetic glucocorticoid receptor agonist that mimics the metabolic, anti-inflammatory, and immunosuppressive activity of the natural glucocorticoids. Amcinonide interacts with specific corticosteroid receptors and was internalized, which leads to binding of DNA and modification of gene expression. This results in synthesis of anti-inflammatory mediators while inhibiting synthesis of inflammatory mediators. Consequently, an overall reduction in chronic inflammation and autoimmune reactions are achieved. Amcinonide can also be classified as a multi-functional small molecule corticosteroid, which has been approved by the FDA and is currently marketed as an ointment, lotion, or cream. It acts as both a transcription factor for responses to glucocorticoids and modulator for other transcription factors while also regulating phospholipase A2 activity.

Mecillinam (INN) or amdinocillin (USAN) is an extended-spectrum penicillin antibiotic that binds specifically to penicillin binding protein 2 (PBP2), and is only considered to be active against Gram-negative bacteria. It is used primarily in the treatment of urinary tract infections, and has also been used to treat typhoid and paratyphoid fever. Because mecillinam has very low oral bioavailability, an orally active prodrug was developed: pivmecillinam. Neither drug is available in the United States.

Amiodarone is categorized as a class III antiarrhythmic agent, and prolongs phase 3 of the cardiac action potential, the repolarization phase where there is normally decreased calcium permeability and increased potassium permeability. It has numerous other effects however, including actions that are similar to those of antiarrhythmic classes Ia, II, and IV. Amiodarone shows beta blocker-like and calcium channel blocker-like actions on the SA and AV nodes, increases the refractory period via sodium- and potassium-channel effects, and slows intra-cardiac conduction of the cardiac action potential, via sodium-channel effects.Amiodarone chemically resembles thyroxine (thyroid hormone), and its binding to the nuclear thyroid receptor might contribute to some of its pharmacologic and toxic actions.

Amisulpride is an atypical antipsychotic used to treat psychosis in schizophrenia and episodes of mania in bipolar disorder. In Italy, it is also used as a treatment for dysthymia. It was introduced by Sanofi-Aventis in the 1990s. Its patent had expired by 2008 and hence generic formulations are now available.Amisulpride function primarily as a D2 and D3 receptor antagonist. It has high affinity for these receptors with dissociation constants of 2.2 nM and 2.4 nM, respectively. Although standard doses used to treat psychosis inhibit dopaminergic neurotransmission, low doses preferentially block inhibitory pre-synaptic autoreceptors.

Amitriptyline, sold under the brand name Elavil among others, is a medication used to treat a number of mental illnesses. This including major depressive disorder and anxiety disorder, and less commonly attention deficit hyperactivity disorder and bipolar disorder. Other uses include prevention of migraines, treatment of neuropathic pain such as fibromyalgia and postherpetic neuralgia, and less commonly insomnia. It is taken by mouth. Common side effects include a dry mouth, trouble seeing, low blood pressure on standing, sleepiness, and constipation.

Amlexanox, also known as AA-673 and CHX 3673, is an anti-inflammatory antiallergic immunomodulator used to treat recurrent aphthous ulcers (canker sores), and (in Japan) several inflammatory conditions. Amlexanox inhibits the synthesis and release of inflammatory mediators, including leukotrienes and histamine, from mast cells, neutrophils, and mononuclear cells. Amlexanox also acts as a leukotriene D4 antagonist and a phosphodiesterase inhibitor. Amlexanox decreases the time ulcers take to heal as well as the pain associated with the ulcers.

Amlodipine (as besylate, mesylate or maleate) is a medication used to lower blood pressure and prevent chest pain. It belongs to a group of medications known as dihydropyridine-type calcium channel blockers. By widening of blood vessels it lowers blood pressure. In angina, amlodipine increases blood flow to the heart muscle to relieve pain due to angina.

Amoxicillin, also spelled amoxycillin and amox, is an antibiotic useful for the treatment of a number of bacterial infections. Amoxicillin is a broad-spectrum semisynthetic antibiotic similar to Ampicillin except that its resistance to gastric acid permits higher serum levels with oral administration. It is the first line treatment for middle ear infections. It may also be used for strep throat, pneumonia, skin infections, and urinary tract infections among others. It is taken orally. This drug acts by inhibiting the synthesis of bacterial cell walls. It inhibits cross-linkage between the linear peptidoglycan polymer chains that make up a major component of the cell walls of both Gram-positive and Gram-negative bacteria. It has two ionizable groups in the physiological range (the amino group in alpha-position to the amide carbonyl group and the carboxyl group).

Ampicillin is an antibiotic used to prevent and treat a number of bacterial infections. This includes respiratory tract infections, urinary tract infections, meningitis, salmonella infections, and endocarditis. It may also be used to prevent group B streptococcal infection in newborns. It is used by mouth, by injection into a muscle, or intravenously. It is not useful for the treatment of viral infections. Ampicillin was developed in 1961. It is on the World Health Organization's List of Essential Medicines, the most important medication needed in a basic health system. Ampicillin is in the penicillin group of beta-lactam antibiotics and is part of the aminopenicillin family. It is roughly equivalent to amoxicillin in terms of activity. Ampicillin is able to penetrate Gram-positive and some Gram-negative bacteria. It differs from penicillin G, or benzylpenicillin, only by the presence of an amino group. That amino group helps the drug penetrate the outer membrane of Gram-negative bacteria. Ampicillin acts as an irreversible inhibitor of the enzyme transpeptidase, which is needed by bacteria to make their cell walls. It inhibits the third and final stage of bacterial cell wall synthesis in binary fission, which ultimately leads to cell lysis; therefore ampicillin is usually bacteriocidal.

Anagrelide (Agrylin/Xagrid, Shire and Thromboreductin, AOP Orphan Pharmaceuticals) is a drug used for the treatment of essential thrombocytosis (ET; essential thrombocythemia), or overproduction of blood platelets. It also has been used in the treatment of chronic myeloid leukemia. Anagrelide works by inhibiting the maturation of platelets from megakaryocytes. The mechanism of action of anagrelide is as a Phosphodiesterase 3 Inhibitor. The physiologic effect of anagrelide is by means of Decreased Platelet Production. Anagrelide is a synthetic quinazoline derivative, Anagrelide reduces platelet production through a decrease in megakaryocyte maturation. Anagrelide inhibits cyclic AMP phosphodiesterase, as well as ADP- and collagen-induced platelet aggregation. At therapeutic doses, it does not influence white cell counts or coagulation parameters. Anagrelide is used for treatment of essential thrombocythemia to reduce elevated platelet counts and the risk of thrombosis.

Anisindione (brand name Miradon) is a synthetic anticoagulant and an indanedione derivative. It prevents the formation of active procoagulation factors II, VII, IX, and X, as well as the anticoagulant proteins C and S, in the liver by inhibiting the vitamin K–mediated gamma-carboxylation of precursor proteins.

Octatropine methylbromide (INN) or anisotropine methylbromide (USAN), trade names Valpin, Endovalpin, Lytispasm and others, is a muscarinic antagonist and antispasmodic. It was introduced to the U.S. market in 1963 as an adjunct in the treatment of peptic ulcer, and promoted as being more specific to the gastrointestinal tract than other anticholinergics. Anisotropine methylbromide is a quaternary ammonium compound. Its use as treatment adjunct in peptic ulcer has been replaced by the use of more effective agents. Depending on the dose, anisotropine methylbromide may reduce the motility and secretory activity of the gastrointestinal system, and the tone of the ureter and urinary bladder and may have a slight relaxant action on the bile ducts and gallbladder. In general, smaller doses of anisotropine methylbromide inhibit salivary and bronchial secretions, sweating, and accommodation; cause dilatation of the pupil; and increase the heart rate. Larger doses are required to decrease motility of the gastrointestinal and urinary tracts and to inhibit gastric acid secretion.

Antazoline is a 1st generation antihistamine with anticholinergic properties used to relieve nasal congestion and in eye drops, usually in combination with naphazoline, to relieve the symptoms of allergic conjunctivitis. Antazoline is an ethylenediamine derivative with histamine H1 antagonistic and sedative properties. Antazoline antagonizes histamine H1 receptor and prevents the typical allergic symptoms caused by histamine activities on capillaries, skin, mucous membranes, and gastrointestinal and bronchial smooth muscles.

Apraclonidine HCl, also known as Iopidine, is a sympathomimetic used in glaucoma therapy. It is an α2-adrenergic agonist and a weak alpha-1 adrenergic receptor agonist. Upon ocular administration, apraclonidine enhances aqueous humor uveoscleral outflow and decreases aqueous production by vasoconstriction.

Aprindine HCl is a Class 1b antiarrhythmic agent used to manage ventricular and supraventricular arrhythmias. In one study, it delayed atrial fibrillation more than digoxin did. It has shown effectiveness when given orally.

Arformoterol tartrate is a long acting beta-adrenoceptor agonist drug indicated for the treatment of chronic obstructive pulmonary disease (COPD). It is sold by Sunovion, under the trade name Brovana, as a solution of arformoterol tartrate to be administered twice daily (morning and evening) by nebulization. It is the active (R,R)-enantiomer of formoterol and was approved by the United States Food and Drug Administration (FDA) on October 6, 2006 for the treatment of COPD.

Atorvastatin is used primarily for lowering blood cholesterol and for prevention of events associated with cardiovascular disease. Like all statins, atorvastatin works by inhibiting HMG-CoA reductase, an enzyme found in liver tissue that plays a key role in production of cholesterol in the body.Atorvastatin is also used for the treatment of dyslipidemia.

Azlocillin Sodium is the sodium salt form of azlocillin, a semisynthetic, extended spectrum acylampicillin with antibacterial activity. Azlocillin binds to penicillin-binding proteins (PBPs) located inside the bacterial cell wall, thereby inhibiting the cross-linkage of peptidoglycans, which are critical components of the bacterial cell wall. This prevents proper bacterial cell wall synthesis, thereby results in the weakening of the bacterial cell wall and eventually leading to cell lysis.

Balsalazide Disodium is the disodium salt form of balsalazide, an aminosalicylate and oral prodrug that is enzymatically cleaved in the colon to produce the anti-inflammatory agent mesalazine. Mesalazine acts locally on the mucosa of the colon where it diminishes inflammation by blocking the production of arachidonic acid metabolites and other inflammatory agents. Balsalazide disodium is used to treat chronic inflammatory bowel disease.

Bendroflumethiazide is a thiazide diuretic used to treat hypertension. Bendroflumethiazide works by inhibiting sodium reabsorption at the beginning of the distal convoluted tubule and may play an important role in the treatment of mild heart failure.

Bentiromide is a peptide used as a screening test for exocrine pancreatic insufficiency and to monitor the adequacy of supplemental pancreatic therapy. It is given by mouth as a noninvasive test. The amount of 4-aminobenzoic acid and its metabolites excreted in the urine is taken as a measure of the chymotrypsin-secreting activity of the pancreas.

Benztropine is a synthetic compound derived from the combination of atropine and diphenhydramine that acts centrally to antagonize M1 muscarinic acetylcholine receptors. Benztropine has been used in the management of Parkinson’s disease symptoms to address involuntary tremor and dystonia. It can also increase the availability of dopamine by inhibiting uptake through the dopamine transporter.

Benzquinamide hydrochloride is a benzquinamide is an antiemetic compound with antihistaminic, mild anticholinergic, and sedative properties. The mechanism of action is not known, but presumably benzquinamide works via antagonism of muscarinic acetycholine receptors and histamine H1 receptors.

Benzthiazide is a research compound with diuretic and antihypertensive properties used in the treatment of high blood pressure and edema.

Betaxolol Hydrochloride is the hydrochloride salt form of betaxolol, a β1-AR selective adrenergic receptor antagonist. Betaxolol hydrochloride acts on the heart and circulatory system and decreases cardiac contractility and rate, and cardiac output levels. When applied topically in the eye, it lowers intraocular pressure by reducing aqueous humor secretion.

Bethanidine sulfate is a guanidinium antihypertensive agent that acts by blocking adrenergic transmission.

Bevantolol Hydrochloride is a beta-1 adrenoceptor antagonist that has been shown to be as effective as other beta blockers for the treatment of angina pectoris and hypertension.

Bifonazole is an imidazole antifungal drug. Bifonazole has dual mode of action. It blocks transformation of 24-methylendihydrolanosterol to desmethylsterol in fungi together with inhibition of HMG-CoA. This enables fungicidal properties against dermatophytes and distinguishes bifonazole from other antifungal drugs. Bifonazole is marketed by Bayer under the trade mark Canespor in ointment form.

Biotin, also known as vitamin H or coenzyme R, is a water-soluble B-vitamin (vitamin B7). It is composed of a ureido (tetrahydroimidizalone) ring fused with a tetrahydrothiophene ring. A valeric acid substituent is attached to one of the carbon atoms of the tetrahydrothiophene ring. Biotin is a coenzyme for carboxylase enzymes, involved in the synthesis of fatty acids, isoleucine, and valine, and in gluconeogenesis.

Bopindolol malonate is a non-selective, potent, long-acting beta adrenoceptor antagonist. It demonstrates inhibition of H2O2-induced lipid peroxdiation. Bopindolol malonate slowly dissociates into the active metabolites 4-(3-tert-butylamino-2-hydroxypropoxy)-2-methyl indole and 4-(3-tert-butylaminopropoxy)-2-carboxyl indole which both demonstrate potent β1-adrenoceptor blocking activity.

Bromfenac is a non-steroidal anti-inflammatory drug (NSAID) marketed in the US as an ophthalmic solution by ISTA Pharmaceuticals for short-term, local use. Prolensa and Bromday are the once-daily formulation of bromfenac, while Xibrom was approved for twice-daily administration. Bromfenac is indicated for the treatment of ocular inflammation and pain after cataract surgery, though it may be prescribed in an off-label manner by the physician. The high degree of penetration and potency of bromfenac can be attributed to the halogenation of the molecule: by adding a bromine moiety the NSAID becomes highly lipophilic which allows for rapid, sustained drug levels in the ocular tissues.

Buclizine is an antihistamine and anticholinergic of the piperazine derivative family. It is considered to be an antiemetic, similar to meclizine.

Bupropion or bupropion hydrochloride, also known formerly as amfebutamone, is a medication primarily used as an antidepressant and smoking cessation aid. It is one of the most frequently prescribed antidepressants in the United States, although in many English-speaking countries, including the United Kingdom, Australia and New Zealand, this is an off-label use. Chemically, bupropion is in the aminoketone family. Bupropion serves as an atypical antidepressant different from most commonly prescribed antidepressants such as selective serotonin reuptake inhibitors (SSRIs). It is an effective antidepressant on its own, but is also popular as an add-on medication in cases of incomplete response to first-line SSRI antidepressants.

Buspirone HCl is an anxiolytic psychotropic drug of the azapirone chemical class. It is primarily used to treat generalized anxiety disorder (GAD). Unlike most drugs predominantly used to treat anxiety, buspirone's pharmacology is not related to benzodiazepines or barbiturates, and so does not carry the risk of physical dependence and withdrawal symptoms for which those drug classes are known.

Butoconazole is an imidazole antifungal used in gynecology. It is administered as a vaginal cream.

Carbachol is a cholinomimetic drug that binds and activates the acetylcholine receptor. Thus it is classified as a cholinergic agonist. It is primarily used for various ophthalmic purposes, such as for treating glaucoma, or for use during ophthalmic surgery. It is generally administered as an ophthalmic solution (i.e. eyedrops).

Carglumic acid is an orphan drug, marketed by Orphan Europe under the trade name Carbaglu. Carglumic acid is used for the treatment of hyperammonaemia in patients with N-acetylglutamate synthase deficiency. The initial daily dose ranges from 100 to 250 mg/kg, adjusted thereafter to maintain normal plasma levels of ammonia.

Carphenazine dimaleate is an antipsychotic agent, mainly used for the treatment of chronic schizophrenia.

Carprofen is a non-steroidal anti-inflammatory drug that veterinarians prescribe as a supportive treatment for various conditions. It provides day-to-day treatment for pain and inflammation from arthritis in geriatric dogs, joint pain, osteoarthritis, hip dysplasia, and other forms of joint deterioration. It is also used to relieve short-term post-operative pain, inflammation, and swelling after spaying, neutering, and other procedures. Carprofen reduces inflammation by inhibition of COX-2 and other sources of inflammatory prostaglandins. This is targeted protection, in that it does not interfere with COX-1 activity.

Cephacetrile is a broad-spectrum first-generation cephalosporin with antibiotic and antibacterial activity. Cephacetrile binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.

Cefaclor is a beta-lactam, second-generation cephalosporin antibiotic that inhibits cell wall synthesis. The antibiotic is active against a wide spectrum of common pathogens, including gram-positive and gram-negative bacteria. Cefaclor binds to and inactivates penicillin-binding proteins (PBP) located in bacterial cytoplasmic membranes. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity.

Cefadroxil is a broad-spectrum antibiotic of the cephalosporin type, effective in Gram-positive and Gram-negative bacterial infections. It is a bactericidal antibiotic. Cefadroxil is a semi-synthetic, beta-lactam, first-generation cephalosporin antibiotic with bactericidal activity. Cefadroxil binds to and inactivates penicillin-binding proteins (PBP) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.

Cefalotin is a first generation cephem antibiotic with a wide range antibacterial activity. The compound is active against gram-positive and gram-negative bacteria, and has been tested in respiratory disease and neuromuscular junction studies.

Cefamandole nafate is a pro-drug that is hydrolyzed by plasma esterases to produce cefamandole, second-generation cephalosporin antibiotic with bactericidal activity. Cefamandole nafate is used to study the effects of expression and inhibition of PBP 2A and other penicillin-binding proteins (PDPs) on bacterial cell wall mucopeptide synthesis. Cefamandole binds to and inactivates penicillin-binding proteins (PBP) located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.

Cefazolin sodium salt inhibits synthesis of bacterial cell wall. Cefazolin Sodium is the sodium salt of cefazolin, a beta-lactam antibiotic and first-generation cephalosporin with bactericidal activity. Cefazolin binds to and inactivates penicillin-binding proteins (PBP) located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity, which results in the weakening of the bacterial cell wall and cell lysis.

Cefepime Hydrochloride is a broad-spectrum cephalosporin with activity against Gram-positive and Gram-negative bacteria. It binds to penicillin-binding proteins and disrupts the cell wall synthesis. It is resistant to hydrolysis by common plasmid and/or chromosomally-mediated β-lactamases. (Last Updated: 02/10/2016).

Cefixime is a third generation cephalosporin antibiotic. It is effective against a variety of Gram-negative bacteria, including E. coli, K. pneumoniae, and H. influenzae. Cefixime binds penicillin-binding proteins and is stable to many penicillinases and β-lactamases. It is an effective, orally-active cephalosporin with applications in acute otitis media, respiratory tract infections, and urinary tract infections.

Cefmetazole is a second-generation, semi-synthetic, beta-lactam cephalosporin antibiotic with antibacterial activity. Cefmetazole binds to penicillin-binding proteins (PBPs) that are responsible for crosslinking of peptidoglycan. By preventing crosslinking of peptidoglycan, cell wall integrity is lost and cell wall synthesis is halted.

Cefonicid Sodium is the sodium salt form of cefonicid, a semisynthetic second-generation broadspectrum cephalosporin with antibacterial activity that inhibits the formation of the bacterial cell wall. Cefonicid binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.

Cefoperazone Sodium is the sodium salt form of cefoperazone and a semi-synthetic, broad-spectrum, beta-lactamase resistant, third-generation cephalosporin antibiotic with bactericidal activity. It is marketed by Pfizer under the name Cefobid. Cefoperazone sodium inhibits bacterial cell wall synthesis by inactivating penicillin binding proteins (PBPs) thereby interfering with the final transpeptidation step required for cross-linking of peptidoglycan units which are a component of bacterial cell walls. This results in a reduction of cell wall stability and causes cell lysis. It is one of few cephalosporin antibiotics effective in treating Pseudomonas bacterial infections which are otherwise resistant to these antibiotics.

Ceforanide is a semi-synthetic, broad-spectrum, beta-lactam, second-generation cephalosporin antibiotic with bactericidal activity. Ceforanide causes inhibition of bacterial cell wall synthesis by inactivating penicillin binding proteins (PBPs) thereby interfering with the final transpeptidation step required for cross-linking of peptidoglycan units which are a component of the cell wall. This results in a reduction of cell wall stability and causes cell lysis.

Cefotaxime Sodium is the sodium salt form of cefotaxime, a beta-lactam, third-generation cephalosporin antibiotic with bactericidal activity. Cefotaxime sodium binds to and inactivates penicillin-binding proteins (PBP) located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linking of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis. Compared to the second and first generation cephalosporins, cefotaxime sodium is more active against gram-negative bacteria and less active against gram-positive bacteria. It is effective against postoperative complications in surgical treatment of pulmonary, tracheal and mediastinal tumors.

Cefotetan Sodium, also known as ICI-156834 and YM-09330, is a second-generation cephalosporin, cephamycin antibiotic that is active against a wide range of both aerobic and anaerobic gram-positive and gram-negative bacteria. Cefotetan binds to penicillin-binding proteins and disrupts the cell wall synthesis.

Cefotetan Hydrochloride is a second-generation cephalosporin that is active against some strains of β-lactamase producing bacteria. It shows anti-microbial activity against Gram-positive and Gram-negative bacteria; it is more efficacious against Gram-negative and anaerobic bacteria. Cefotetan Hydrochloride binds to penicillin-binding proteins and disrupts the cell wall synthesis.

Cefoxitin Sodium is a semisynthetic cephamycin antibiotic resistant to beta-lactamase. It is derived from Cephamycin C and is highly resistance to β-lactamase inactivation. Also an antibacterial, cefoxitin sodium acts by adhering to bacterial penicillin-binding proteins, thereby inhibiting cell wall synthesis.

Cefpodoxime Proxetil is an antibacterial with a broad spectrum activity. It is an oral, third generation cephalosporin, ester prodrug of the active free acid metabolite Cefpodoxime. It is active against most Gram-positive and Gram-negative organisms. It is commonly used to treat acute otitis media, pharyngitis, sinusitis, and gonorrhea. It also finds use as oral continuation therapy when intravenous cephalosporins (such as ceftriaxone) are no longer necessary for continued treatment. Currently, it is only marketed as generic preparations in the USA.

Cefprozil, under the marketed trade name Cefzil, is a second-generation cephalosporin type antibiotic. It can be used to treat bronchitis, ear infections, skin infections, and other bacterial infections. It comes as a tablet and as a liquid suspension. Cefprozil's effect is dependent on its binding to penicillin-binding proteins (PBPs) located in the bacterial cytoplasmic membrane. Binding results in the inhibition of the transpeptidase enzymes, thereby preventing cross-linking of the pentaglycine bridge with the fourth residue of the pentapeptide and interrupting consequent synthesis of peptidoglycan chains. As a result, cefprozil inhibits bacterial septum and cell wall synthesis formation.

Ceftazidime is a broad-spectrum β-lactam antibiotic used as an antimicrobial agent. It is used for treating febrile neutropenia in patients with cancer. It is a third-generation cephalosporin. As a class, cephalosporins have activity against Gram-positive and Gram-negative bacteria. The balance of activity tips toward Gram-positive organisms for earlier generations; later generations of cephalosporins have more Gram-negative coverage. Ceftazidime is one of the few in this class with activity against Pseudomonas.

Ceftizoxime is third generation cephalosporin effective against Gram-negative and Gram-positive bacteria. It binds penicillin-binding proteins (PBPs) and inhibits the bacterial cell wall synthesis. Unlike other third-generation cephalosporins, the whole C-3 side chain in ceftizoxime has been removed to prevent deactivation by hydrolytic enzymes. It rather resembles cefotaxime in its properties, but is not subject to metabolism.

Ceftriaxone sodium is an antibiotic, a third-generation cephalosporin. Like other third-generation cephalosporins, it has broad-spectrum activity against Gram-positive bacteria and expanded Gram-negative coverage compared to second-generation agents. This includes pneumonia, ear infections, skin infections, urinary tract infections, gonorrhea, pelvic inflammatory disease, septisis, bone and joint infections, intra-abdominal infections, and meningitis. It is also used preoperatively to reduce the risk of postoperative infections. It is administered by intravenous or intramuscular injection.

Cefuroxime sodium is a broad-spectrum cephalosporin antibiotic useful in infections of gram-negative and gram-positive organisms, gonorrhea, and haemophilus.

Cephalexin is a cephalosporin antibiotic used to study the effect of expression, binding, and inhibition of PBP3 and other penicillin-binding proteins on bacterial cell wall mucopeptide synthesis. Cephalexin disrupts the synthesis of the peptidoglycan layer of bacterial cell walls which is responsible for cell wall structural integrity. Peptidoglycan synthesis is facilitated by transpeptidases known as penicillin-binding proteins.

Cefaloglycin is a first-generation semisynthetic cephalosporin with antibacterial activity. Cephaloglycin binds to and inactivates penicillin-binding proteins located on the inner membrane of the bacterial cell wall. This results in the weakening of the bacterial cell wall and causes cell lysis.

Chlorhexidine digluconate solution is a bis-biguanide family cationic broad spectrum antibiotic. Studies indicate that chlorhexidine digluconate solution functions, via destabilization of the outer bacterial membrane, which resulted in the release of periplasmic enzymes in gram negative bacteria. In addition, Chlorhexidine digluconate solution inhibits oxygen utilization which leads to a reduction in bacterial ATP. Furthermore, Chlorhexidine digluconate solution is very effective against bacteria such as Propionibacterium, Selenomonas, and cocci resembling Veillonella.

Chloroprocaine Hydrochloride is a synthetic, local anesthetic agent. At the injection site, chloroprocaine hydrochloride acts by inhibiting sodium influx through binding to specific membrane sodium ion channels in the neuronal cell membranes, restricting sodium permeability, and blocking nerve impulse conduction. This leads to a loss of sensation. Chloroprocaine hydrochloride is short-acting due to rapid hydrolysis by pseudocholinesterase into para-aminobenzoic acid in plasma.

Chloropyramine is a first generation antihistamine drug approved for the treatment of allergic conjunctivitis, allergic rhinitis, bronchial asthma, and other atopic (allergic) conditions. Chloropyramine is known as a competitive reversible H1-receptor antagonist, meaning that it exerts its pharmacological action by competing with histamine for the H1 subtype histamine receptor. By blocking the effects of histamine, the drug inhibits the vasodilation, increased vascular permeability, and tissue edema associated with histamine release in the tissue.

Chloroxine is a synthetic antibacterial agent. It inhibits the growth of Gram-positive and some Gram-negative bacteria and also induces SOS-DNA repair. Chlorxine shows bacteriostatic, fungistatic and antiprotozoal effects in vivo.

Chlorpropamide is a drug in the sulfonylurea class used to treat type 2 diabetes mellitus. It is a long-acting 1st generation sulfonylurea. Chlorpropamide acts to increase the secretion of insulin, so it is only effective in patients who have some pancreatic beta cell function.

Cinalukast is a potent, selective CysLT1 (LTD4) leukotriene receptor antagonist. It is used in the treatment of asthma, cinalukast selectively antagonizes leukotriene D4 (LTD4) at the cysteinyl leukotriene receptor, CysLT1, in the human airway. Cinalukast inhibits the actions of LTD4 at the CysLT1 receptor, preventing airway edema, smooth muscle contraction, and enhanced secretion of thick, viscous mucus.

Cinitapride is a gastroprokinetic agent and medication prescribed to treat conditions caused by an overactive digestive tract. It slows the actions of the muscles to reduce the symptoms of conditions such as acid reflux, ulcer dyspepsia, and delayed gastric emptying. It acts as an agonist of the 5-HT1 and 5-HT4 receptors and as an antagonist of the 5-HT2 receptors.

Cinolazepam is a benzodiazepine derivative drug. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Due to its strong sedative properties, it is primarily used as an hypnotic.

Cinoxacin was an older synthetic antimicrobial related to the quinolone class of antibiotics with activity similar to oxolinic acid and nalidixic acid. It was commonly used thirty years ago to treat urinary tract infections in adults. There are reports that cinoxacin had also been used to treat initial and recurrent urinary tract infections and bacterial prostatitis in dogs however this veterinary use was never approved by the FDA. In complicated UTI, the older gyrase-inhibitors such as cinoxacin are no longer indicated.

Ciprofloxacin hydrochloride is a broad-spectrum antimicrobial carboxyfluoroquinoline, an fluoroquinolone antibiotic that is widely used as an antimicrobial and immunomodulatory agent. It is capable of inducing respiratory, urinary tract, gastrointestinal, and abdominal infections. It functions by inhibiting DNA gyrase (a type II topoisomerase) and topoisomerase IV, the enzymes responsible for negative supercoiling of chromosomes and DNA strand separation, thus blocking initiation of bacterial replication. Most recently ciprofloxacin has been used in the management of postexposure inhalational anthrax and radiation combined injury resulting from nuclear disasters.

Clavulanate potassium is an acid which is a suicide inhibitor of bacterial beta-lactamase enzymes from Streptomyces clavuligerus. Administered alone, it has only weak antibacterial activity against most organisms, but when combined with penicillin-group antibiotics it prevents antibiotic inactivation by microbial lactamase. It is commonly combined with amoxicillin or ticarcillin.