masofaniten + enzalutamide + androgen deprivation therapy

This combination therapy, evaluated in the Phase 2 EXTRA-PC trial (NCT06312670) led by Dr. Pedro Barata, consists of masofaniten (EPI-7386), enzalutamide, and standard androgen deprivation therapy (ADT) for the treatment of metastatic hormone-sensitive prostate cancer (mHSPC). Masofaniten is an investigational, first-in-class oral small molecule that inhibits the androgen receptor (AR) by binding to its N-terminal domain (NTD), potentially overcoming resistance associated with mutations or splice variants in the ligand-binding domain (LBD). Enzalutamide is an established AR signaling inhibitor that targets the LBD. The triplet approach was designed to provide more comprehensive AR blockade by targeting two distinct regions of the receptor while simultaneously suppressing systemic testosterone levels. However, the trial was terminated early in late 2024 following ESSA Pharma's decision to halt the development and production of masofaniten due to insufficient efficacy in other prostate cancer trials.

Brand names

Xtandi

Other names

EPI-7386 + enzalutamide + ADTmasofaniten + enzalutamide + ADTEXTRA-PC regimen