fludelone

Fludelone is a synthetic, third-generation epothilone analog and microtubule-stabilizing agent developed at Memorial Sloan-Kettering Cancer Center. As a 16-membered macrocyclic lactone, it is designed to overcome the limitations of taxanes, such as poor water solubility and susceptibility to multidrug resistance (MDR) mediated by P-glycoprotein. Fludelone promotes the polymerization of tubulin into stable microtubules, leading to cell cycle arrest at the G2/M phase and subsequent apoptosis. Preclinical studies have demonstrated its potent antitumor activity across a wide range of human xenograft models, including breast, colon, lung, and ovarian cancers. Notably, fludelone has shown the ability to achieve "therapeutic cure" (complete remission without relapse) in drug-resistant and refractory tumors. It exhibits improved pharmacokinetic properties compared to earlier epothilones and can be administered both intravenously and orally.

Other names

Iso-oxazole fludelone20-desmethyl-20-fluoro-epothilone B