Clinical data | |
---|---|
Other names | EPI-7386 |
Routes of administration | By mouth |
Drug class | N-Terminal domain antiandrogen |
Identifiers | |
| |
CAS Number | |
PubChem CID | |
UNII | |
ChEMBL | |
Chemical and physical data | |
Formula | C24H24Cl2N4O4S |
Molar mass | 535.44 g·mol−1 |
3D model (JSmol) | |
| |
|
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 2 3 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.
- 1 2 3 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.
- 1 2 3 4 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.
- ↑ 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.; Zhang, J.; Saad, F.; Villaluna, K.; Younginger, B.; Le Moigne, R.; Cesano, A. (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.
This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.