Bicalutamide: Difference between revisions

Bicalutamide, marketed as Casodex <ref name="ARA prostate">PMID: 24639562</ref><ref name="nonsteroidal">PMID: 16841196</ref>, is one of the most stable and tolerated Androgen receptor antagonist (ARA) used in the treatment of prostate cancer <ref name="ARA prostate" /><ref name="bicalutamide">PMID: 15833816</ref><ref name="AAWS">PMID: 28971898</ref>, belonging to the first generation of antiandrogens developed <ref name="ARA prostate" /><ref name="MoA">PMID: 35245614</ref>.  

It is a competitive antagonist <ref name="Bicalutamide functions">PMID: 12015321</ref><ref name="MoA" /><ref name="AAWS" /> which binds to the LBD producing a transcriptionally inactive AR <ref name="Bicalutamide functions" />. However, it seems that the long-term use of these drugs and other first generation antiandrogens lead to withdrawal syndrome in prostate cancer resistant to castration patients <ref name="ARA prostate" /><ref name="nonsteroidal" />. In many cases, associated AR mutations, like W741L, can switch the mechanism of action of the drug from antagonist to agonist or partial agonist <ref name="ARA prostate" /><ref name="bicalutamide" /><ref name="nonsteroidal" /><ref name="Unexpected">PMID: 21506597</ref><ref name="MoA">PMID: 35245614</ref>.