ESSA Pharma presents the updated phase 1 Masofaniten clinical data at the 2024 ASCO Genitourinary Cancers Symposium. Masofaniten (EPI-7386) is a first-in-class investigational, N-terminal domain (NTD) androgen receptor (AR) inhibitor under development for prostate cancer. The androgen receptor (AR) signaling pathway is responsible for growth and survival of most prostate cancers. Unlike present therapies by binding to the ligand-binding domain (LBD) of AR and inducing drug resistance, Masofaniten offers a unique mechanism that inhibits AR activity through targeting the N-terminal domain (NTD) of the AR and suppresses AR transcriptional activation.
Masofaniten is studied with Enzalutamide in the phase 1/2 clinical trial for metastatic castration-resistant prostate cancer (mCRPC) patients on androgen deprivation therapy and naïve to second-generation antiandrogens.