patupilone

Patupilone is a 16-membered ring macrolide belonging to the epothilone class of anticancer agents. It is a natural secondary metabolite isolated from the myxobacterium Sorangium cellulosum. Patupilone acts as a microtubule stabilizer by binding to the αβ-tubulin heterodimer subunit at the same site as paclitaxel (taxol), promoting tubulin polymerization and stabilizing microtubules. This leads to inhibition of microtubule function, cell cycle arrest at the G2-M transition phase, and ultimately apoptosis of cancer cells. Patupilone was investigated for use in various cancers including ovarian cancer, lung cancer, brain cancer, breast cancer, gastric cancer, colorectal cancer and prostate cancer. Despite promising preclinical activity and early-phase clinical trials showing some tumor control in heavily pretreated patients with metastatic disease (notably colorectal and ovarian cancers), later-stage trials failed to demonstrate significant efficacy or survival benefit over standard therapies; development was discontinued due to lack of efficacy and high toxicity[1][3][5][6][8][10].

Other names

epothilone BEPO906EPO-906EPO 906