Products
Cabazitaxel is released as a concentrate for the preparation of an infusion solution. It has been approved in many countries since 2011 (Jevtana).
Structure and properties
Cabazitaxel (C45H57NO14, Mr = 835.9 g/mol) is a taxane semisynthetically derived from a constituent of yew needles. It is structurally closely related to docetaxel, which is itself a derivative of paclitaxel. Two hydroxy groups have been replaced by methoxy groups. Cabazitaxel exists as a white crystalline powder that is virtually insoluble in water due to its high lipophilicity.
Effects
Cabazitaxel (ATC L01CD) has antineoplastic and cytotoxic properties. The effects are due to disruption of the microtubule network and inhibition of cell division, leading to cell death. Unlike paclitaxel and docetaxel, cabazitaxel is not a substrate of P-glycoprotein, which plays an important role in the development of resistance of tumor cells to cytostatic drugs. Therefore, it is also better absorbed into the brain across the blood–brain barrier, which may be an advantage in the treatment of central lesions.
Indications
In combination with prednisone or prednisolone for the treatment of patients with hormone-refractory metastatic prostate cancer who are pretreated with a docetaxel-based regimen.
Contraindications
For complete precautions, see the drug label.
Interactions
Cabazitaxel is metabolized by CYP3A4 and inhibits CYP3A4. Corresponding interactions are possible. Cabazitaxel should not be co-administered with live vaccines.
Adverse effects
The most common adverse effects include anemia, leukopenia, neutropenia, thrombocytopenia, and diarrhea.
