GLPG3667 is an oral, reversible, and selective tyrosine kinase 2 (TYK2) inhibitor. It is being developed to treat inflammatory and auto-immune diseases. Biochemical assays showed that GLPG3667 displayed nanomolar potency on TYK2 with a selectivity over other JAK kinases >3-fold. In human PBMC, GLPG3667 showed comparable potency on the IFNα and IL-23 pathways (around 50 nM). Selectivity for TYK2 on the IFNα pathway was >14-fold and >19-fold toward the IL-2 and GM-CSF pathways in human PBMC and whole blood, respectively. Dermal ear inflammation in a mouse model of psoriasis driven by IL-23 was prevented by GLPG3667 with a minimal effective dose of 3 mg/kg given orally once daily. This effect was associated with a decrease in neutrophil infiltration and STAT3 phosphorylation at sites of inflammation. In healthy HV, GLPG3667 completely inhibited IFNα-induced STAT1 and STAT3 phosphorylation but did not impact IL-2- and GM-CSF-induced STAT5 phosphorylation.

ZH8667 is a trace amine-associated receptor 1 (TAAR1)–Gs agonist.

L-608 is a novel ionizable amino lipid designed for formulating lipid nanoparticles (LNPs) to enable efficient subcutaneous (s.c.) delivery of mRNA therapeutics. Engineered to address inflammation associated with mRNA LNPs, L608 integrates seamlessly with steroid prodrugs, such as budesonide-C16 and budesonide-C18:1, to suppress local and systemic inflammatory responses while prolonging therapeutic protein expression. Preclinical studies demonstrate that L608 LNPs significantly reduce injection-site edema (>80% improvement) and lower systemic inflammatory markers (e.g., haptoglobin), while achieving 2–3× higher plasma AUC for proteins like hFGF21 compared to non-steroid LNPs.

4’-α-C-Methyluridine represents a structurally modified uridine analog with significant pharmacological potential. As a nucleoside derivative, it shares structural similarities with uridine—a compound recognized for its ​antiepileptic properties—while offering enhanced metabolic stability through its methyl modification.

Certolizumab pegol (Certolizumab) is a recombinant, polyethylene glycolylated, antigen-binding fragment of a humanized monoclonal antibody that selectively targets and neutralizes tumour necrosis factor-α (TNF-α).

Quisovalimab (AVTX-002; AEVI 002; SAR 252067) is a human monoclonal antibody against LIGHT, a tumor necrosis factor (TNF)-related cytokine (TNFSF14) that plays an important role in acute respiratory distress syndrome (ARDS) and cytokine release syndrome (CRS) COVID-19. Quisovalimab can be used in COVID-19 acute respiratory distress syndrome and other studies.

Belimumab (LymphoStat B) is a humanized IgG1λ monoclonal antibody against B-lymphocyte stimulator (BLyS) protein. Belimumab antagonizes BLyS activity in autoimmune diseases and B-lymphocyte malignancies. Belimumab can be used for systemic lupus erythematosus (SLE) research.

Tabalumab (LY2127399) is a human anti-BAFF (B-cell activating factor) monoclonal antibody (IgG4 type) with neutralising activity against membrane bound and soluble BAFF. Tabalumab can be used in studies of autoimmune diseases such as rheumatoid arthritis, renal failure and systemic lupus erythematosus.

Zigakibart (BION-1301) is an IgG4-kappa, anti-TNFSF13 (tumor necrosis factor (TNF) superfamily member 13, APRIL, CD256) humanized monoclonal antibody. Zigakibart shows anti-inflammatory activity.

Sibeprenlimab (VIS649) is a humanized IgG2 monoclonal antibody which inhibits a proliferation-inducing ligand (APRIL). Sibeprenlimab suppresses pathogenic immunoglobulins (IgA and IgM), while preserving antibody responses to mRNA-based vaccines against SARS-COV-2. Sibeprenlimab reduces urinary protein-to-creatinine ratio (UPCR) and glomerular filtration rate (GFR). Sibeprenlimab is promising for the research of IgA nephropathy (IgAN).

Urelumab, a fully human, non-ligand binding, CD137 agonist IgG4 monoclonal antibody, enhances T-cell and natural killer-cell antitumor activity, and may enhance cytotoxic activity of Rituximab (HY-P9913). Urelumab can be used for the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and other types of non-Hodgkin lymphoma (NHL).

Utomilumab (PF 05082566) is a fully human IgG2 mAb agonist of the T-cell costimulatory receptor 4-1BB/CD137. Utomilumab can be used for the research of relapsed/refractory follicular lymphoma (FL) and other CD20+ non-Hodgkin lymphomas (NHL).

Brentuximab is a monoclonal antibody targeting CD30. Brentuximab is conjugated with monomethyl auristatin E (MMAE) (HY-15162) to form the antibody-drug conjugate Brentuximab vedotin (HY-P99107), which can induce apoptosis in primary effusion lymphoma cells. Brentuximab vedotin exhibits antitumor activity with an IC50 of 10 nM against human CD30+ cancer cells.

Varlilumab (CDX-1127) is a first-in-class human IgG1 anti-CD27 monoclonal antibody. Varlilumab has an anti-tumor activity.

Mitazalimab (ADC-1013; JNJ-64457107) is FcγR-dependent CD40 agonist with tumor-directed activity. Mitazalimab activates antigen-presenting cells, e.g. dendritic cells (DC), to initiate tumor-reactive T cells. Therefore, Mitazalimab induces tumor-specific T cells to infiltrate and kill tumors. Mitazalimab remodels the tumor-infiltrating myeloid microenvironment.

Bleselumab (ASKP 1240) is a human anti-CD40 monoclonal antibody (mAb). Bleselumab binds to human CD40 with high affinity (Kd: ?0.24?nM). Bleselumab inhibits immune responses by blocking the interaction of CD40 with its ligand CD40L. Bleselumab prevents organ transplant rejection.

Iscalimab (CFZ-533) is a non-depleting IGg1 monoclonal antibody targeting CD40 (KD: 0.3 nM). Iscalimab can be used for research of Graves' hyperthyroidism and autoimmune diseases.

AV-105 is a tosylate precursor compound derived from ​Florbetapir (18F), a radiolabeled styrylpyridine derivative referenced in ​patent WO2010078370A1 (Example 1.5). This precursor plays a crucial role in the synthesis of ​18F-radiolabeled imaging agents, particularly for ​positron emission tomography (PET) applications.

AZ-5104 is a pharmacologically active metabolite derived from the demethylation of ​AZD9291 (osimertinib). It functions as a ​potent EGFR inhibitor, demonstrating strong inhibitory activity against various ​EGFR mutants and ​ErbB4.

ML162 is a covalent inhibitor that specifically targets ​glutathione peroxidase 4 (GPX4), a key regulator of ferroptosis. This compound exhibits ​selective cytotoxicity against cancer cell lines harboring ​mutant RAS oncogenes, making it a promising candidate for precision oncology.

A83B4C63 is a highly potent small-molecule inhibitor targeting the DNA repair enzyme polynucleotide kinase 3'-phosphatase (PNKP), exhibiting strong binding affinity with a ​Kd of 80 nM. Due to its limited aqueous solubility, A83B4C63 was formulated into ​nano-encapsulated carriers, enhancing its therapeutic potential—particularly in ​PTEN-deficient colorectal cancer (CRC).

Furamidine dihydrochloride (NSC 305831) tyrosyl-DNA phosphodiesterase (Tdp1), also is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with IC50 of 9.4 uM.