Taltobulin (HTI-286) is a synthetic tripeptide cysteine analog, an effective antimicrotubule agent. It inhibits tumor cell growth in vitro (IC₅₀: 0.2-7.3 nM for various cell lines) and in vivo (1.6 mg/kg i.v. inhibits human tumor xenografts; 3 mg/kg p.o. inhibits Lox melanoma and KB-3-1 epidermoid xenografts). It induces mitotic arrest and apoptosis, avoiding P-glycoprotein-mediated drug resistance.
