Wikipedia

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] 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] Masofaniten shows 20-fold higher antiandrogenic potency than ralaniten in vitro (IC50Tooltip Half-maximal inhibitory concentration = 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]

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
PubChem CID
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

References

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  1. ^ a b c 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.
  2. ^ a b c 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.
  3. ^ a b c d 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.
  4. ^ 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.
  5. ^ 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.


 

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