Drug intelligence / Profile preview

EPI-7386 + abiraterone acetate + prednisone

Development stage
Unknown
Lead developer
ESSA Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

**EPI-7386 + abiraterone acetate + prednisone** is a combination therapy under clinical investigation for metastatic castration-resistant prostate cancer (mCRPC) and high-risk metastatic castration-sensitive prostate cancer (mCSPC)[1][3][5][7]. EPI-7386 is an investigational, highly-selective, oral, small molecule inhibitor that targets the N-terminal domain of the androgen receptor, a site distinct from existing antiandrogens, designed to block androgen receptor transcriptional activity even in the presence of resistance mechanisms such as mutations in the ligand-binding domain[1][9]. Abiraterone acetate is a CYP17 inhibitor, widely approved as a hormonal therapy for prostate cancer, that blocks androgen biosynthesis[1]. Prednisone is included to counteract mineralocorticoid excess due to abiraterone's mechanism. This combination provides dual blockade of androgen receptor signaling: EPI-7386 inhibits AR activity at the N-terminal domain, while abiraterone suppresses androgen production. Prednisone is used to manage side effects related to abiraterone therapy. The combination is primarily investigated in men with mCRPC and mCSPC and is sponsored by ESSA Pharma in collaboration with Janssen[1][3][5][7].

Other names
abirateroneprednisone
02

Targets

CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)GR (Glucocorticoid receptor)AR (Adrenergic receptors)

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