Cabazitaxel

Cabazitaxel (kuh-BA-zih-TAK-sil) is a drug used with prednisone to treat hormone-resistant prostate cancer that has spread and that had been treated with docetaxel. It is also being studied in the treatment of other types of cancer. Cabazitaxel blocks cell growth by stopping cell division and may kill cancer cells. It is a type of antimitotic agent. Also called Jevtana and taxoid XRP6258.

Information about Cabazitaxel

Cabazitaxel is a taxane and antineoplastic agent which is currently used in the therapy of castration-resistant metastatic prostate cancer after failure of docetaxel. 

Liver safety of Cabazitaxel

Therapy with cabazitaxel has been associated with a low rate of serum enzyme elevations, but has not been linked to cases of clinically apparent acute liver injury. 

Mechanism of action of Cabazitaxel

Cabazitaxel (cab" a zi tax' el) is a semisynthetic derivative of a natural taxoid and contains a complex diterpenoid molecular structure with a central 8-member taxane ring.  The taxoids were initially isolated from bark of the Western Yew tree (Taxus breviflora) and found to have antitumor activity in high throughput assays.  Their mechanism of anticancer activity appears to be due to their binding to intracellular microtubulin which prevents the disassembly of cytoskeletal microtubules, preventing cell division and leading to cell death.  Cabazitaxel was developed when it was found to have low affinity for P-glycoprotein, a common mediator of docetaxel resistance.  Thus, cabazitaxel was evaluated initially in patients with docetaxel resistant tumors.  Cabazitaxel was found to prolong survival in men with castration-resistant, metastatic prostate cancer not responding to docetaxel therapy. 

FDA approval information for Cabazitaxel

It was approved for this use in combination with oral prednisolone in the United States in 2010. 

Dosage and administration for Cabazitaxel

Cabazitaxel is available in single dose vials of 60 mg/mL under the brand names Jevtana.  Cabazitaxel, like other taxanes, is administered intravenously, in an initial dose of 25 mg/m2 as a one hour infusion every three weeks.  Cabazitaxel must be diluted to a concentration of 10 mg/mL before administration and should be given with oral prednisolone in a dose of 10 mg daily throughout the period of cabazitaxel treatment. 

Side effects of Cabazitaxel

Side effects are common and require close monitoring and expert management; they include myelosuppression and diarrhea which can be severe, as well as nausea, vomiting, mucositis, fatigue, bone-, muscle- and back-pain, skin rash, alopecia, nail changes, neuropathy, fluid retention, phlebitis, cardiomyopathy, infusion site reactions, and hypersensitivity reactions.

 

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