Cevipabulin (TTI-237) fumarate is a microtubule-active antitumor compound and inhibits the binding of [3H] vinblastine to tubulin (IC50: 18-40 nM in the human tumor cell line).

Microtubule (human tumor cells):18-40 nM

Cevipabulin (0-50 nM, 72 hours) exhibits potent activity (IC50s: 18-40 nM) on ovarian, breast, prostate, and cervical tumor cell lines. At low concentrations (20-40 nM), it induces sub-G1 nuclei, while concentrations above 50 nM result in a significant G2-M block [1].

In mice, Cevipabulin ( 5, 10, 15, and 20 mg/kg, every 4 days for 4 cycles; i.v. and p.o.) is active against human tumor xenografts and showing dose-dependent effects, with good antitumor activity at 20 and 15 mg/kg [1].