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][4] 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).^[2][3][4] 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.^[2][3][4] It was planned to enter phase I clinical 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]

Other namesEPI-7386

Routes of
administrationBy mouth

Drug classN-Terminal domain antiandrogen

CAS Number

• 2416716-62-4

Quick facts Clinical data, Other names ...

Masofaniten

Clinical data
Other names	EPI-7386
Routes of administration	By mouth
Drug class	N-Terminal domain antiandrogen
Identifiers
IUPAC name N-[4-[[4-[2-[3-chloro-4-(2-chloroethoxy)-5-cyanophenyl]propan-2-yl]phenoxy]methyl]pyrimidin-2-yl]methanesulfonamide
CAS Number	2416716-62-4
PubChem CID	146484310
ChemSpider	115275789
UNII	OQ2SF7P8B2
ChEMBL	ChEMBL5095106
Chemical and physical data
Formula	C24H24Cl2N4O4S
Molar mass	535.44 g·mol−1
3D model (JSmol)	Interactive image
SMILES 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 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

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