RPR258063

RPR258063 is a **small molecule drug** developed as the primary **active metabolite of ombrabulin (AVE8062)**, a vascular disrupting agent (VDA) designed for oncology indications, specifically for the treatment of solid tumors including breast, esophageal, ovarian, and prostate cancers. It acts as a **modulator of tubulin**, disrupting microtubule function in tumor vascular endothelial cells, leading to a rapid shutdown of the tumor blood supply and subsequent tumor necrosis. The drug was the subject of several clinical pharmacokinetic studies, which observed biphasic or triphasic elimination (terminal half-life ~8 hours)[1][3][4]. Preclinical and early clinical development was collaboratively handled by Ajinomoto and Sanofi[4].

Other names

1H-Pyrrole-1-carboxamide, 3-ethyl-2,5-dihydro-4-methyl-N-[2-[4-[(trans-4-methylcyclohexyl)aminocarbonylaminosulfonyl]phenylethyl]-2-oxo-trans-3-Ethyl-2,5-dihydro-4-methyl-N-[2-[4-[[(trans-4-methylcyclohexyl)amino]carbonyl]amino]sulfonyl]phenyl]ethyl]-2-oxo-1H-pyrrole-1-carboxamide1-[[p-[2-(3-Ethyl-4-methyl-2-oxo-3-pyrroline-1-carboxamido)ethyl]phenyl]sulfonyl]-3-(trans-4-methylcyclohexyl)urea]