Desmethylenzalutamide

Desmethylenzalutamide

Desmethylenzalutamide is a biologically active metabolite of the antiandrogen drug enzalutamide. It is formed in the body by the cytochrome P450 enzyme CYP2C8 and has similar antiandrogenic activity to enzalutamide.

Pharmacology

Desmethylenzalutamide acts as a competitive antagonist of the androgen receptor, preventing androgens such as testosterone and dihydrotestosterone from binding to and activating the receptor. This inhibits the growth of prostate cancer cells, which are often dependent on androgens for survival and proliferation.

Metabolism

Desmethylenzalutamide is formed from enzalutamide in the body by the action of the enzyme CYP2C8. This is a form of phase I metabolism, which often results in the formation of active metabolites. The formation of desmethylenzalutamide can be inhibited by CYP2C8 inhibitors, which may affect the efficacy of enzalutamide treatment.

Clinical significance

Desmethylenzalutamide has similar antiandrogenic activity to enzalutamide and contributes to the overall effect of the drug in the treatment of prostate cancer. The levels of desmethylenzalutamide in the body can be affected by factors such as the presence of CYP2C8 inhibitors, which may need to be considered in the clinical use of enzalutamide.

See also

• Enzalutamide
• Androgen receptor
• Prostate cancer