Desmethylapalutamide

Desmethylapalutamide

Desmethylapalutamide is a nonsteroidal antiandrogen (NSAA) that is used in the treatment of prostate cancer. It is a major active metabolite of apalutamide, which is an antiandrogen medication that is used in the same context. Desmethylapalutamide is primarily used in the treatment of non-metastatic castration-resistant prostate cancer (NM-CRPC).

Pharmacology

Desmethylapalutamide, like apalutamide, works by binding to the androgen receptor (AR) and inhibiting its interaction with androgens. This prevents the activation of the AR and subsequent upregulation of androgen-responsive genes. In prostate cancer, this can slow the growth of cancer cells and can even lead to cell death.

Clinical Use

Desmethylapalutamide is used in the treatment of NM-CRPC. This is a stage of prostate cancer where the cancer has not spread to other parts of the body (non-metastatic), but continues to grow despite low levels of testosterone in the body (castration-resistant). Desmethylapalutamide is used in combination with a gonadotropin-releasing hormone (GnRH) analog or surgical castration.

Side Effects

Common side effects of desmethylapalutamide include fatigue, joint pain, rash, decreased appetite, weight loss, and hypertension. More serious side effects can include falls, fractures, and seizures.

See Also

• Apalutamide
• Nonsteroidal antiandrogen
• Prostate cancer