Cabazitaxel is a semi-synthetic microtubule inhibitor belonging to the taxane class of chemotherapeutic agents. It is a second-generation taxane specifically indicated for the treatment of metastatic castration-resistant prostate cancer (mCRPC) in patients previously treated with a docetaxel-containing regimen. Unlike other taxanes, cabazitaxel is a poor substrate for the P-glycoprotein (P-gp) efflux pump, allowing it to retain activity in docetaxel-resistant tumors. It is administered as an intravenous infusion every three weeks in combination with oral prednisone.
Adult: The recommended dose is 20 mg/m² (or 25 mg/m² per some protocols, based on tolerability and clinical judgement) administered as a one-hour intravenous infusion every 3 weeks, in combination with oral prednisone 10 mg daily throughout treatment.
Note: 1. MUST be diluted prior to infusion. The 60 mg/0.947 mL concentrate must be diluted in the entire contents of the provided solvent (5.7 mL of 5.8% ethanol in water) within the vial. This solution must then be further diluted into a 250 mL infusion bag of either 0.9% Sodium Chloride Injection or 5% Dextrose Injection to achieve a final concentration of 0.10 to 0.26 mg/mL. 2. Administer as a one-hour IV infusion using a 0.22 micrometer in-line filter. 3. Premedication: Administer IV antihistamine (e.g., diphenhydramine 25 mg or equivalent H1 antagonist), IV H2 antagonist (e.g., ranitidine 50 mg), and IV corticosteroid (e.g., dexamethasone 8 mg or equivalent) at least 30 minutes prior to each infusion. Oral antiemetics are also recommended.
Cabazitaxel binds to and stabilizes tubulin within microtubules, inhibiting their depolymerization and disassembly. This stabilization disrupts the normal dynamic reorganization of the microtubule network that is essential for vital interphase and mitotic cellular functions. The drug promotes the assembly of stable microtubules and induces abnormal bundles of microtubules in the cell, leading to a blockade in the G2/M phase of the cell cycle and ultimately, apoptotic cell death.
Pregnancy: Category D. Cabazitaxel can cause fetal harm when administered to a pregnant woman based on its mechanism of action and animal data showing embryolethality and teratogenicity. Women of childbearing potential should be advised to use effective contraception during and for 6 months after treatment. Men with female partners of childbearing potential should use effective contraception during and for 3 months after treatment.
Driving: May cause fatigue, dizziness, or blurred vision. Patients should be cautioned about driving or operating machinery if they experience these effects.
| Ketoconazole, Itraconazole, Voriconazole, Clarithromycin | Strong CYP3A4 inhibitors increase cabazitaxel plasma concentration, increasing risk of severe toxicity (neutropenia). | Major - Contraindicated/Requires dose avoidance. |
| Rifampicin, Phenytoin, Carbamazepine, St. John's Wort | Strong CYP3A4 inducers decrease cabazitaxel plasma concentration, potentially reducing efficacy. | Major - Avoid combination or consider dose adjustment. |
| Other myelosuppressive agents (e.g., Capecitabine, other chemotherapies) | Additive risk of severe bone marrow suppression. | Major - Requires enhanced monitoring of blood counts. |
| Live Vaccines (e.g., MMR, Varicella, Yellow Fever) | Risk of disseminated infection due to immunosuppression. | Major - Contraindicated during treatment. |
Same composition (Cabazitaxel (60mg/ml)), different brands: