masofaniten

Masofaniten (formerly known as EPI-7386) is a first-in-class, investigational, highly selective oral small molecule inhibitor of the androgen receptor (AR) N-terminal domain. It belongs to a new class of compounds called "anitens," which inhibit AR activity by binding to the N-terminal domain rather than the ligand-binding domain targeted by other AR pathway inhibitors such as enzalutamide. This unique mechanism allows masofaniten to block AR-driven gene transcription even in cases where resistance has developed due to point mutations or splice variants affecting the ligand-binding domain. Masofaniten has demonstrated potent anti-tumor activity in preclinical models and early clinical trials for metastatic castration-resistant prostate cancer (mCRPC), including efficacy against tumors driven by resistant AR variants like AR-V7. The drug was developed primarily for use in mCRPC patients who have progressed on standard therapies.

Other names

masofanitenEPI-7386EPI7386EPI 7386