N-Desmethylapalutamide

N-Desmethylapalutamide is an active metabolite of apalutamide, a nonsteroidal antiandrogen which is used in the treatment of prostate cancer. It was identified as the major metabolite of apalutamide in humans and has been found to possess equivalent antiandrogenic activity to that of apalutamide itself.

Pharmacology

N-Desmethylapalutamide, like apalutamide, works by binding to the androgen receptor (AR) and preventing its activation and subsequent upregulation of androgen-responsive genes by androgens like testosterone and dihydrotestosterone (DHT). It is described as a "pure" antiandrogen, meaning that it does not have the capacity to activate the AR under normal physiological circumstances.

Clinical significance

The clinical significance of N-Desmethylapalutamide is that it may contribute to the clinical efficacy of apalutamide in the treatment of prostate cancer. It has similar potency and efficacy to apalutamide in terms of AR antagonism, and circulates at higher concentrations than apalutamide. As such, it may be responsible for a significant portion of the total antiandrogenic activity of apalutamide.

See also

• List of investigational sex-hormonal agents

N-Desmethylapalutamide Resources
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