EPI-7386 + apalutamide

EPI-7386 + apalutamide is a combination therapy under clinical investigation for the treatment of prostate cancer. EPI-7386 is an orally bioavailable, small molecule inhibitor that targets the N-terminal domain (NTD) of the androgen receptor (AR), preventing AR-driven gene transcription even in the context of ligand independent AR activation. Apalutamide is an androgen receptor antagonist that inhibits AR nuclear translocation and AR-mediated transcription. This combination seeks to more comprehensively inhibit AR signaling by targeting both the ligand-binding domain (with apalutamide) and the N-terminal domain (with EPI-7386), potentially overcoming mechanisms of resistance to second-generation anti-androgen therapies. The combination is being tested particularly in metastatic castration-resistant prostate cancer (mCRPC) and non-metastatic castration-resistant prostate cancer (nmCRPC) or metastatic castration-sensitive prostate cancer (mCSPC)[1][2][4].

Other names

EPI-7386 plus apalutamideEPI7386 plus apalutamideEPI 7386 plus apalutamide