Drug intelligence / Profile preview

cabazitaxel + gemcitabine

Development stage
Discontinued
Lead developer
Sanofi
Modality
Small Molecules
Administration
Intravenous
01

Overview

**cabazitaxel + gemcitabine** is an investigational combination of two cytotoxic chemotherapeutic agents intended for the treatment of advanced, metastatic, or unresectable solid tumors. *Cabazitaxel* is a second-generation taxane that inhibits microtubule depolymerization, promoting mitotic arrest; it is approved for metastatic castration-resistant prostate cancer. *Gemcitabine* is a pyrimidine nucleoside analog that inhibits DNA synthesis, targeting cells in S-phase and the G1/S checkpoint, and is approved for multiple malignancies. The mechanisms of these drugs are complementary, with activity at different points of the cell cycle. Clinical evaluation (Phase I) of their combination in refractory solid tumors revealed unacceptably high hematologic toxicity (not sequence-dependent), including neutropenia and thrombocytopenia. No maximum tolerated dose (MTD) could be established, and further development was discontinued for this combination due to safety concerns, despite preliminary evidence of antitumor activity in some cases[1][2].

02

Targets

DNA polymerase familyRNR (Ribonucleotide reductase)TUBB (Tubulin (alpha and beta subunits))

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