Biochem/physiol Actions

Cevipabulin (TTI-237) is a potent microtubule-stabilizing agent that binds to tubulin vinblastine binding site, a typical site of binding for microtubule-destabilizing agents. It is likely that cevipabulin, similarly to other triazolopyrimidines, promotes longitudinal tubulin contacts in microtubules, which promotes stabilization of micro-tubule. Cevipabulin exhibits potent cytotoxic activity in cancer cell lines including cell line expressing a high level of P-glycoprotein. It is active in vivo in several mouse xenograft models of human cancer.