EPI-7386

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EPI-7386
Clinical data
Routes of
administration
By mouth
Drug classN-Terminal domain antiandrogen

EPI-7386 is an N-terminal domain antiandrogen, or antagonist of the N-terminal domain (NTD) of the androgen receptor (AR), which is under development for the treatment of prostate cancer.[1][2][3] The compound was developed as a successor of previous drugs in the EPI series such as EPI-001, ralaniten (EPI-002), and ralaniten acetate (EPI-506).[1][2][3] EPI-7386 shows 20-fold higher antiandrogenic potency than ralaniten in vitro (IC50 = 535 nM vs. 9,580 nM, respectively), as well as greater stability in human hepatocytes.[1][2][3] It is planned to enter phase I clinical trials in 2020.[3]

References[edit]

  1. ^ a b c Le Moigne R, Banuelos CA, Mawji NR, Tam T, Wang J, Jian K, et al. (2020). "IND candidate EPI-7386 as an N-terminal domain androgen receptor inhibitor in development for the treatment of prostate cancer". Journal of Clinical Oncology. 38 (6_suppl): 142. doi:10.1200/JCO.2020.38.6_suppl.142. S2CID 213003338.
  2. ^ a b c Moigne R, Zhou HJ, Mawji NR, Banuelos CA, Wang J, Jian K, et al. (2019). "Next generation N-terminal domain androgen receptor inhibitors with improved potency and metabolic stability in castration-resistant prostate cancer models". Journal of Clinical Oncology. 37 (7_suppl): 220. doi:10.1200/JCO.2019.37.7_suppl.220. ISSN 0732-183X. S2CID 88047727.
  3. ^ a b c d Sadar MD (May 2020). "Discovery of drugs that directly target the intrinsically disordered region of the androgen receptor". Expert Opinion on Drug Discovery. 15 (5): 551–560. doi:10.1080/17460441.2020.1732920. PMC 8693730. PMID 32100577. S2CID 211523793.