Masofaniten Explained

Masofaniten, also known by its developmental code name 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). Masofaniten shows 20-fold higher antiandrogenic potency than ralaniten in vitro (= 535 nM vs. 9,580 nM, respectively), as well as greater stability in human hepatocytes. It was planned to enter phase I clinical trials in 2020. Preliminary results of a phase I/II clinical trial were published in 2023.[4] [5]

Notes and References

  1. Le Moigne R, Banuelos CA, Mawji NR, Tam T, Wang J, Jian K, Andersen RJ, Cesano A, Sadar M, Zhou HJ, Virsik P . 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 . 2020 . 142 . 10.1200/JCO.2020.38.6_suppl.142 . 213003338 .
  2. Moigne R, Zhou HJ, Mawji NR, Banuelos CA, Wang J, Jian K, Virsik P, Andersen RJ, Sadar M . 88047727. 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. 2019. 220. 0732-183X. 10.1200/JCO.2019.37.7_suppl.220.
  3. Sadar MD . Discovery of drugs that directly target the intrinsically disordered region of the androgen receptor . Expert Opinion on Drug Discovery . 15 . 5 . 551–560 . May 2020 . 32100577 . 10.1080/17460441.2020.1732920 . 8693730 . 211523793 .
  4. Laccetti AL, Chatta GS, Iannotti N, Kyriakopoulos C, Villaluna K, Le Moigne R, Cesano A . Phase 1/2 study of EPI-7386 in combination with enzalutamide (enz) compared with enz alone in subjects with metastatic castration-resistant prostate cancer (mCRPC). . Journal of Clinical Oncology . 41 . 6_suppl . 2023-02-20 . 0732-183X . 10.1200/JCO.2023.41.6_suppl.179 . 179. 257549466 .
  5. Laccetti AL, Chatta G, Kyriakopoulos C, Iannotti N, Hotte SJ, Markowski MC, Pili R, Vuky J, Zhang J, Saad F, Villaluna K . 1813P Phase I/II trial of oral EPI-7386 in combination with enzalutamide (enz) compared to enz alone in metastatic castration-resistant prostate cancer (mCRPC) subjects: Current phase I (PI) results . Annals of Oncology . 34 . 2023 . 10.1016/j.annonc.2023.09.2761 . S982–S983. 264383200 .

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