| Description: |
Phase I study of Cevipabulin: Twenty-eight patients were enrolled and treated with TTI-237 at dose of 4.5, 9, 15, 22.5 and 31.5 mg/m(2). One dose-limiting toxicity neutropenia fever was observed at 31.5 mg/m(2), and all seven patients developed grade 3 or 4 neutropenia at that dose level. TTI-237 dosage was de-escalated to 22.5 and 18 mg/m(2). Six patients were treated at the 18 mg/m(2) dose level without dose-limiting toxicity prior to trial termination. The mean terminal-phase elimination half-life (t(1/2)) for TTI-237 was 25-29 h, and the mean area under the concentration time curve at 31.5 mg/m(2) was 2,768 ng•h/mL. Conclusion: A protocol defined maximum tolerated dose was not determined because of early termination of the TTI-237 trial by the sponsor. 18 mg/m(2) may be a tolerable dose of TTI-237. (source: Invest New Drugs. 2012 Feb;30(1):266-72.)
Preclinical study of Cevipabulin (TTI-237): Cevipabulin (TTI-237) appears to bind at the vinca site, but exhibits some properties similar to those of taxane-site ligands, such as enhancing tubulin polymerization. The compound works against a variety of tumors, including those resistant to paclitaxel and vincristine. Furthermore, cevipabulin is stable and water-soluble, and can be administered i.v. or p.o. in saline. It can be synthesized in bulk quantities efficiently. Based on these properties, cevipabulin was selected for clinical development. (source: Methods Find Exp Clin Pharmacol. 2009 Sep;31(7):443-7.)For the detailed information of Cevipabulin, the solubility of Cevipabulin in water, the solubility of Cevipabulin in DMSO, the solubility of Cevipabulin in PBS buffer, the animal experiment (test) of Cevipabulin, the cell expriment (test) of Cevipabulin, the in vivo, in vitro and clinical trial test of Cevipabulin, the EC50, IC50,and affinity,of Cevipabulin, Please contact DC Chemicals. |
