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[edit | edit source]
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[edit | edit source]
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[edit | edit source]
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[edit | edit source]
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