Cabazitaxel

Cabazitaxel (Jevtana) is a semi-synthetic derivative of a natural taxoid. Cabazitaxel (Jevtana) increases CYP3A enzyme activities in rat hepatocytes. The mean ex-vivo human plasma protein binding of Cabazitaxel (Jevtana) is 91.6%. Cabazitaxel (Jevtana) is rapidly and extensively metabolised into numerous metabolites. Cabazitaxel (Jevtana) demonstrates activity in several murine and human resistant cell lines. With a 4-day exposure to cabazitaxel, cytotoxicity is noted with relatively low cabazitaxel concentrations. Cabazitaxel (Jevtana) shows high antitumor activity in 3 human colorectal cell lines (HCT-116, HCT-8, and HT-29). In accompanying models, Cabazitaxel (Jevtana) has significant antitumor activity. In murine tumor xenografts (colon C38 and pancreas P03), Cabazitaxel (Jevtana) causes complete tumor regressions. Using SF-295 and U251 human glioblastoma cell lines, both orthotopic and subcutaneous murine xenografts are generated. Cabazitaxel (Jevtana) treatment leads to complete regression in the majority of subcutaneously implanted tumors. Cabazitaxel (Jevtana) has entered in a phase I clinical trial in the treatment of solid cancer. Cabazitaxel (Jevtana) plus Prednisone, Carboplatin has entered in a phase II clinical trial in the treatment of prostate cancer. Cabazitaxel is a semi-synthetic derivative of a natural taxoid.