Taltobulin hydrochloride (HTI-286 hydrochloride), a synthetic analogue of the tripeptide hemiasterlin, effectively bypasses P-glycoprotein-mediated resistance both in vitro and in vivo as a robust antimicrotubule agent. It prevents the polymerization of purified tubulin, destabilizes cellular microtubule structures, and triggers both mitotic arrest and apoptosis [1].