tasidotin

Tasidotin is a third-generation, synthetic, water-soluble pentapeptide analog of the marine depsipeptide dolastatin 15. It acts as an antimitotic and antineoplastic agent by targeting microtubules. Tasidotin and its major metabolite, tasidotin C-carboxylate, suppress the dynamic instability of microtubules primarily by reducing their shortening rate (disassembly), decreasing the frequency of switching from growth to shortening (catastrophe frequency), and reducing the time spent in growth phases. This leads to inhibition of cell proliferation. Unlike other microtubule-targeted drugs that inhibit polymerization or stabilize plus ends, tasidotin uniquely enhances dynamic instability at minus ends while suppressing it at plus ends. Tasidotin was developed as an orally active derivative for cancer therapy and has been studied in phase II clinical trials for advanced or metastatic non-small cell lung carcinoma, hormone-refractory prostate cancer, and melanoma.

Brand names

Synthadotin

Other names

tasidotinatasidotine