ortataxel

Ortataxel is a semisynthetic, second-generation taxane derivative with potential antineoplastic activity. It binds to and stabilizes tubulin molecules, interfering with the dynamics of microtubule assembly and disassembly, which results in inhibition of cell division and cellular proliferation. Ortataxel is notable for being a poor substrate for P-glycoprotein (Pgp), multi-drug resistance protein (MRP1), and breast cancer resistance protein (BCRP) mediated efflux, allowing it to modulate multi-drug resistance mechanisms. This property may make it useful for treating tumors that are resistant to other taxanes due to overexpression of these efflux proteins. Ortataxel has been investigated in clinical trials for various cancers including lymphoma, lung cancer (notably non-small cell lung cancer), glioblastoma, kidney cancer (renal cell carcinoma), metastatic breast cancer resistant to taxanes, and solid tumors[1][2][3][5][7]. It was originally developed by Indena and the State University of New York; development was later continued by Spectrum Pharmaceuticals before transitioning to Assertio Therapeutics. The drug reached phase II clinical trials in several indications but has since been discontinued for all known indications[5][7]. Its oral bioavailability distinguishes it from some other taxanes.

Other names

ortataxel