EPI-7386 is an ''N''-terminal domain antiandrogen, or

antagonist An antagonist is a character in a story who is presented as the chief foe of the protagonist. Etymology The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, riv ...

of the ''N''-terminal domain (NTD) of the

androgen receptor The androgen receptor (AR), also known as NR3C4 (nuclear receptor subfamily 3, group C, member 4), is a type of nuclear receptor that is activated by binding any of the androgenic hormones, including testosterone and dihydrotestosterone in th ...

(AR), which is under development for the treatment of

prostate cancer Prostate cancer is cancer of the prostate. Prostate cancer is the second most common cancerous tumor worldwide and is the fifth leading cause of cancer-related mortality among men. The prostate is a gland in the male reproductive system that sur ...

. The compound was developed as a successor of previous drugs in the EPI series such as

EPI-001 EPI-001 is the first inhibitor of the androgen receptor amino-terminal domain. The single stereoisomer of EPI-001, EPI-002, is a first-in-class drug that the USAN council assigned a new stem class "-aniten" and the generic name "ralaniten". This ...

ralaniten Ralaniten (developmental code name EPI-002) is an N-terminal domain antiandrogen which was never marketed. It is a derivative (chemistry), derivative of bisphenol A and one of the four stereoisomers of EPI-001. A prodrug of ralaniten, ralaniten ac ...

(EPI-002), and

ralaniten acetate Ralaniten acetate (developmental code name EPI-506) is a first-in-class antiandrogen that targets the ''N''-terminal domain (NTD) of the androgen receptor (AR) developed by ESSA Pharmaceuticals and was under investigation for the treatment of p ...

(EPI-506). EPI-7386 shows 20-fold higher antiandrogenic

potency Potency may refer to: * Potency (pharmacology), a measure of the activity of a drug in a biological system * Virility * Cell potency, a measure of the differentiation potential of stem cells * In homeopathic dilutions, potency is a measure of how ...

than ralaniten '' in vitro'' ( = 535 nM vs. 9,580 nM, respectively), as well as greater stability in human hepatocytes. It is planned to enter

phase I Phase 1, Phase I or Phase One may refer to: Media * Marvel Cinematic Universe: Phase One, six American superhero films from 2008–2012 * ''Phase One'' (Art Ensemble of Chicago album), 1971 * ''Phase One'' (Saga album), 1998 * ''Phase One'', r ...

clinical trials in 2020.

References

Experimental cancer drugs Nonsteroidal antiandrogens {{genito-urinary-drug-stub