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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
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] The compound was developed as a successor of previous drugs in the EPI series such asEPI-001,ralaniten (EPI-002), andralaniten acetate (EPI-506).[1][2][3] 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.[1][2][3] It was planned to enterphase Iclinical trials in 2020.[3] Preliminary results of a phase I/II clinical trial were published in 2023.[4][5]

References

[edit]
  1. ^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.
  2. ^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.
  3. ^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.
  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.
ARTooltip Androgen receptor
Agonists
SARMsTooltip Selective androgen receptor modulator
Antagonists
GPRC6A
Agonists


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