cabazitaxel

Cabazitaxel is a chemotherapy medication in the taxane class. It is a semi-synthetic derivative of paclitaxel that acts as a microtubule inhibitor by binding to beta-tubulin and stabilizing microtubules, which disrupts mitosis and promotes cancer cell death.

Indications and use: Cabazitaxel is approved for metastatic castration-resistant prostate cancer (mCRPC) in patients who have previously received docetaxel therapy. It is marketed under the brand name Jevtana. In clinical practice, it is used as a second-line taxane therapy after progression on or after docetaxel.

Administration and regimen: The drug is given by intravenous infusion every three weeks. A typical regimen is cabazitaxel 25 mg/m2 every 3 weeks, with an oral prednisone regimen (commonly 5 mg twice daily) started with cycle 1. Treatment continues until disease progression or unacceptable toxicity. Premedication with antiemetics and close monitoring for hematologic toxicity are common components of care.

Mechanism of action and resistance: As a taxane, cabazitaxel stabilizes microtubules, inhibiting cell division. It has activity in some taxane-resistant tumors, in part due to a distinct binding profile and reduced susceptibility to drug efflux pumps such as P-glycoprotein, contributing to its efficacy after prior taxane therapy.

Adverse effects and safety: The most important toxicities are hematologic, particularly neutropenia and febrile neutropenia, followed by fatigue, diarrhea, nausea, vomiting, decreased appetite, stomatitis, and neuropathy. Infections, hypersensitivity reactions, and rash can occur. Dose modifications may be required for hepatic impairment or in the context of significant drug interactions.

Pharmacology and interactions: Cabazitaxel is primarily metabolized by hepatic CYP3A enzymes. Co-administration with strong CYP3A inhibitors or inducers can alter exposure and may necessitate dose adjustments or avoidance.