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Non-steroidal antiandrogen

Nonsteroidal antiandrogen
Drug class
Bicalutamide.svg
Bicalutamide, the most widely used nonsteroidal antiandrogen and the most widely used antiandrogen in prostate cancer.
Class identifiers
Synonyms Nonsteroidal androgen receptor antagonists
Use Prostate cancer; Acne; Hirsutism; Seborrhea; Pattern hair loss; Hyperandrogenism; Transgender hormone therapy; Male precocious puberty; Priapism
ATC code L02BB
Biological target Androgen receptor
Chemical class Nonsteroidal

A nonsteroidal antiandrogen (NSAA) is an antiandrogen with a nonsteroidal chemical structure. They are typically selective and full or silent antagonists of the androgen receptor (AR) and act by blocking the effects of androgens like testosterone and dihydrotestosterone (DHT). SAAs are used in the treatment of androgen-dependent conditions in men and women. They are the converse of steroidal antiandrogens (SAAs), which are antiandrogens that are steroids and are structurally related to testosterone.

SAAs are used in clinical medicine for the following indications:

Unlike SAAs, NSAAs have little or no capacity to activate the AR, show no off-target hormonal activity such as progestogenic, glucocorticoid, or antimineralocorticoid activity, and lack antigonadotropic effects. For these reasons, they have improved efficacy and selectivity as antiandrogens and do not lower androgen levels, instead acting solely by directly blocking the actions of androgens at the level of their biological target, the AR.

Nonsteroidal androgen synthesis inhibitors like can also be described as "NSAAs", although the term is usually reserved to describe AR antagonists.

Seviteronel (VT-464) is a nonsteroidal androgen biosynthesis inhibitor which is under development for the treatment of prostate cancer.



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