Products
Enzalutamide was initially registered in capsule form (Xtandi). Film-coated tablets were approved in many countries in 2019. They are smaller and therefore easier to take. Enzalutamide was approved in the United States in 2012 and in many countries and the EU in 2013.
Structure and properties
Enzalutamide (C21H16F4N4O2S, Mr = 464.4 g/mol) is an imidazolidine derivative. It exists as a white crystalline powder that is practically insoluble in water. Enzalutamide is one of the nonsteroidal antiandrogens.
Effects
Enzalutamide (ATC L02BX) is a selective and highly potent antagonist at the androgen receptor that abolishes the effects of the androgens testosterone and dihydrotestosterone. It also has an effect on signaling and inhibits translocation of the receptor to the nucleus. Enzalutamide inhibits tumor proliferation, induces cell death of cancer cells, reduces tumor volume, and can prolong survival by several months. It has an active metabolite (-desmethylenzalutamide) and a long half-life of several days.
Indications
In combination with GnRH analogs for the treatment of patients with metastatic castration-resistant prostate cancer in progression on or after docetaxel therapy.
Dosage
According to the SmPC. The drug is taken once daily and independently of meals.
Contraindications
- Hypersensitivity
- Pregnancy, due to fertility damaging properties
Full precautions can be found in the drug label.
Interactions
Enzalutamide is metabolized by CYP2C8 and CYP3A4 and is an inducer of CYP3A4, CYP2C9, and CYP2C19. Corresponding drug-drug interactions are possible and must be considered during treatment.
Adverse effects
The most common possible adverse effects include joint pain, back pain, muscle pain, diarrhea, fatigue, edema, flushing, infection, and headache.
