Chemistry:Masofaniten
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][4] 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).[2][3][4] Masofaniten 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.[2][3][4] It was planned to enter phase I clinical trials in 2020.[4] Preliminary results of a phase I/II clinical trial were published in 2023.[5][6] The development of masofaniten was discontinued in 2024 following disappointing clinical trial results.[1][7]
References
- ↑ 1.0 1.1 "Masofaniten". 9 October 2025. https://adisinsight.springer.com/drugs/800056122.
- ↑ 2.0 2.1 2.2 "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. 2020. doi:10.1200/JCO.2020.38.6_suppl.142.
- ↑ 3.0 3.1 3.2 "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. 2019. doi:10.1200/JCO.2019.37.7_suppl.220. ISSN 0732-183X.
- ↑ 4.0 4.1 4.2 4.3 "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. doi:10.1080/17460441.2020.1732920. PMID 32100577.
- ↑ "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): 179. 2023-02-20. doi:10.1200/JCO.2023.41.6_suppl.179. ISSN 0732-183X.
- ↑ "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: S982–S983. 2023. doi:10.1016/j.annonc.2023.09.2761.
- ↑ Rashid, Ayesha (4 November 2024). "ESSA Pharma Pulls Plug on Masofaniten Prostate Cancer Drug After Disappointing Trial Results Against Xtandi". https://xtalks.com/essa-pharma-pulls-plug-on-masofaniten-prostate-cancer-drug-after-disappointing-trial-results-against-xtandi-3936/.
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