Clascoterone (cortexolone 17alpha-propionate; CB-03-01; Winlevi; Breezula) is a novel and potent androgen antagonist that has been approved in 2020 for topical use in the treatment of acne.

Enzalutamide (formerly MDV3100; MDV-3100; trade name: Xtandi) is an orally bioavailable, 2nd-generation and non-steroidal androgen-receptor (AR) antagonist with potential antineoplastic activity.

Spironolactone (SC9420; SC-9420; SC 9420; Spiresis; Spiridon) is a potent androgen receptor/AR antagonist with potential antineoplastic activity.

AC-262536 (AC262536) is a novel selective androgen receptor modulator (SARM) with beneficial anabolic effects.

MK-0773 (PF-05314882) is a novel and potent SARM (selective androgen receptor modulator) that binds to AR with an IC50 of 6.6 nM and with the potential for the prevention and treatment of muscle wasting associated with cancer.

S-23 is a novel and potent nonsteroidal agonist.

YK-11 is a novel, potent, synthetic, steroidal selective androgen receptor modulator (SARM) that acts as a partial agonist of androgen receptor with osteogenic activity.

BMS-564929 is a novel, highly potent, orally bioactive, nonsteroidal tissue selective androgen receptor (AR) modulator that binds to androgen receptor (AR) with a Ki of 2.11±0.16 nM.

LY2452473 is a novel, potent, selective and orally bioavailable androgen receptor modulator (SARM) with potential tissue-selective androgenic/anti-androgenic activity.

N-Desmethyl Apalutamide is the CYP2C8 and CYP3A4-mediated, N-demethylated and active metabolite of Apalutamide, but the potency is less than the parent drug. Apalutamide (JNJ-56021927; ARN-509; Erleada) is an approved anticancer drug that acts as an AR/androgen receptor inhibitor.