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Masofaniten

From Wikipedia, the free encyclopedia
Anti-cancer drug

Pharmaceutical compound
Masofaniten
Clinical data
Other namesEPI-7386
Routes of
administration
By mouth
Drug classN-Terminal domain antiandrogen
Identifiers
  • N-[4-[[4-[2-[3-chloro-4-(2-chloroethoxy)-5-cyanophenyl]propan-2-yl]phenoxy]methyl]pyrimidin-2-yl]methanesulfonamide
CAS Number
PubChemCID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC24H24Cl2N4O4S
Molar mass535.44 g·mol−1
3D model (JSmol)
  • CC(C)(C1=CC=C(C=C1)OCC2=NC(=NC=C2)NS(=O)(=O)C)C3=CC(=C(C(=C3)Cl)OCCCl)C#N
  • InChI=1S/C24H24Cl2N4O4S/c1-24(2,18-12-16(14-27)22(21(26)13-18)33-11-9-25)17-4-6-20(7-5-17)34-15-19-8-10-28-23(29-19)30-35(3,31)32/h4-8,10,12-13H,9,11,15H2,1-3H3,(H,28,29,30)
  • Key:GVCZSODXLFBYSS-UHFFFAOYSA-N

Masofaniten, also known by its developmental code nameEPI-7386, is anN-terminal domain antiandrogen, orantagonist of theN-terminal domain (NTD) of theandrogen receptor (AR), which is under development for the treatment ofprostate cancer.[1][2][3][4] The compound was developed as a successor of previous drugs in the EPI series such asEPI-001,ralaniten (EPI-002), andralaniten acetate (EPI-506).[2][3][4] Masofaniten shows 20-fold higherantiandrogenicpotency than ralanitenin vitro (IC50Tooltip Half-maximal inhibitory concentration = 535 nM vs. 9,580 nM, respectively), as well as greater stability in humanhepatocytes.[2][3][4] It was planned to enterphase Iclinical 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

[edit]
  1. ^ab"Masofaniten".AdisInsight. 9 October 2025. Retrieved15 October 2025.
  2. ^abcLe 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.
  3. ^abcMoigne 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.
  4. ^abcdSadar 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.
  5. ^Laccetti AL, Chatta GS, Iannotti N, Kyriakopoulos C, Villaluna K, Le Moigne R, et al. (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.doi:10.1200/JCO.2023.41.6_suppl.179.ISSN 0732-183X.S2CID 257549466.
  6. ^Laccetti AL, Chatta G, Kyriakopoulos C, Iannotti N, Hotte SJ, Markowski MC, 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.S2CID 264383200.
  7. ^Rashid A (4 November 2024)."ESSA Pharma Pulls Plug on Masofaniten Prostate Cancer Drug After Disappointing Trial Results Against Xtandi".Xtalks. Retrieved15 October 2025.
ARTooltip Androgen receptor
Agonists
SARMsTooltip Selective androgen receptor modulator
Antagonists
GPRC6A
Agonists


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