pofenbrodib + abiraterone acetate

This combination drug consists of **pofenbrodib**, a highly selective small molecule inhibitor of the bromodomain proteins CREB-binding protein (CBP) and p300, and **abiraterone acetate**, a prodrug of abiraterone which is an inhibitor of the enzyme CYP17A1 involved in androgen biosynthesis. Abiraterone acetate is established in the management of metastatic castration-resistant prostate cancer (mCRPC) by blocking androgen biosynthesis and is approved in combination with corticosteroids such as prednisone. Pofenbrodib acts by inhibiting gene transcription programs important for tumor growth via CBP/p300 bromodomain inhibition, which disrupts androgen receptor (including AR-v7 variant) coactivation. The combination is under investigation for its potential synergistic efficacy in mCRPC, leveraging the suppression of androgen signaling from abiraterone acetate and interference with transcriptional coactivators by pofenbrodib[2][4][6][8]. Pathos is the main developer for pofenbrodib in this setting, while abiraterone acetate is developed and marketed by Janssen Biotech.

Brand names

Zytiga

Other names

pocenbrodibabiraterone acetate