Chemistry:EPI-7386
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Short description: Anti-cancer drug
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| Other names | EPI-7386 |
| Routes of administration | By mouth |
| Drug class | N-Terminal domain antiandrogen |
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| Formula | C24H24Cl2N4O4S |
| Molar mass | 535.44 g·mol−1 |
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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).[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 was planned to enter phase I clinical trials in 2020.[3] Preliminary results of a phase I/II clinical trial were published in 2023.[4][5]
References
- ↑ 1.0 1.1 1.2 "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.
- ↑ 2.0 2.1 2.2 "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.
- ↑ 3.0 3.1 3.2 3.3 "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.
- ↑ Laccetti, Andrew Leonard; Chatta, Gurkamal S.; Iannotti, Nicholas; Kyriakopoulos, Christos; Villaluna, Karen; Le Moigne, Ronan; Cesano, Alessandra (2023-02-20). "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): 179–179. doi:10.1200/JCO.2023.41.6_suppl.179. ISSN 0732-183X.
- ↑ Laccetti, A.L.; Chatta, G.; Kyriakopoulos, C.; Iannotti, N.; Hotte, S.J.; Markowski, M.C.; Pili, R.; Vuky, J. et al. (2023). "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. doi:10.1016/j.annonc.2023.09.2761.
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