N-Desmethylapalutamide
N-Desmethylapalutamide is a nonsteroidal antiandrogen (NSAA) that is a major active metabolite of the drug apalutamide. It is used in the treatment of prostate cancer. N-Desmethylapalutamide is formed in the body through the metabolism of apalutamide by the cytochrome P450 enzyme CYP2C8.
Pharmacology[edit | edit source]
N-Desmethylapalutamide acts as an androgen receptor (AR) antagonist. It binds to the AR and inhibits the action of androgens, which are male sex hormones such as testosterone and dihydrotestosterone (DHT). This inhibition prevents the growth of prostate cancer cells that rely on androgens for proliferation.
Metabolism[edit | edit source]
The conversion of apalutamide to N-Desmethylapalutamide is primarily mediated by the enzyme CYP2C8. This metabolic pathway is significant because N-Desmethylapalutamide retains similar pharmacological activity to its parent compound, apalutamide, contributing to the overall therapeutic effects.
Clinical Significance[edit | edit source]
N-Desmethylapalutamide, as an active metabolite, plays a crucial role in the efficacy of apalutamide in treating prostate cancer. Understanding its pharmacokinetics and pharmacodynamics is important for optimizing treatment regimens and managing potential drug interactions.
See also[edit | edit source]
References[edit | edit source]
External links[edit | edit source]
Search WikiMD
Ad.Tired of being Overweight? Try W8MD's physician weight loss program.
Semaglutide (Ozempic / Wegovy and Tirzepatide (Mounjaro / Zepbound) available.
Advertise on WikiMD
WikiMD's Wellness Encyclopedia |
Let Food Be Thy Medicine Medicine Thy Food - Hippocrates |
Translate this page: - East Asian
中文,
日本,
한국어,
South Asian
हिन्दी,
தமிழ்,
తెలుగు,
Urdu,
ಕನ್ನಡ,
Southeast Asian
Indonesian,
Vietnamese,
Thai,
မြန်မာဘာသာ,
বাংলা
European
español,
Deutsch,
français,
Greek,
português do Brasil,
polski,
română,
русский,
Nederlands,
norsk,
svenska,
suomi,
Italian
Middle Eastern & African
عربى,
Turkish,
Persian,
Hebrew,
Afrikaans,
isiZulu,
Kiswahili,
Other
Bulgarian,
Hungarian,
Czech,
Swedish,
മലയാളം,
मराठी,
ਪੰਜਾਬੀ,
ગુજરાતી,
Portuguese,
Ukrainian
Medical Disclaimer: WikiMD is not a substitute for professional medical advice. The information on WikiMD is provided as an information resource only, may be incorrect, outdated or misleading, and is not to be used or relied on for any diagnostic or treatment purposes. Please consult your health care provider before making any healthcare decisions or for guidance about a specific medical condition. WikiMD expressly disclaims responsibility, and shall have no liability, for any damages, loss, injury, or liability whatsoever suffered as a result of your reliance on the information contained in this site. By visiting this site you agree to the foregoing terms and conditions, which may from time to time be changed or supplemented by WikiMD. If you do not agree to the foregoing terms and conditions, you should not enter or use this site. See full disclaimer.
Credits:Most images are courtesy of Wikimedia commons, and templates, categories Wikipedia, licensed under CC BY SA or similar.
Contributors: Prab R. Tumpati, MD