Zosuquidar trihydrochloride

A potent P-glycoprotein (P-gp) inhibitor with Ki of 60 nM; fully restores sensitivity to vinblastine, doxorubicin, etoposide, and Taxol in CEM/VLB100 cells at 0.1 uM; enhances the antitumor activity of Taxol in a MDR human non-small cell lung carcinoma nude mouse xenograft model.Blood Cancer Phase 3 Discontinued (In Vitro) :Zosuquidar (0.3 μM; 48 h) enhances the cytotoxicity of DNR (substrates for P-glycoproteins) in P-glycoproteins active cell lines.Zosuquidar (5-16 μM; 72 h) treatment alone shows high cytotoxic concentration to drug-sensitive and MDR cell lines. (In Vivo) :Zosuquidar (intraperitoneal injection; 30, 10, 3, or 1 mg/kg; once daily; 5 d) treatment shows a significant increase in life span.Zosuquidar (intraperitoneal injection; 30 mg/kg; once daily; 5 d) treatment shows the potentiation with a combined of Doxorubicin.