abiraterone acetate + apalutamide

**Abiraterone acetate + apalutamide** is a combination of two oral small molecule drugs, each targeting the androgen signaling pathway in prostate cancer through distinct mechanisms. Abiraterone acetate is a prodrug of abiraterone, an inhibitor of CYP17A1, a key enzyme in androgen biosynthesis, thereby reducing production of androgens both within the tumor and systemically. Apalutamide is a nonsteroidal androgen receptor (AR) antagonist that directly binds the ligand-binding domain of the AR, inhibiting its nuclear translocation and DNA binding, thus blocking transcriptional activation of AR-responsive genes. This combination has been investigated especially in **metastatic castration-resistant prostate cancer (mCRPC)**, with clinical trials showing additive efficacy due to simultaneous suppression of androgen biosynthesis and AR-mediated signaling[1][2][3][5]. The combination is typically administered with prednisone for corticosteroid support and to mitigate mineralocorticoid excess from abiraterone[1][2][3].

Brand names

Erleada + Zytiga

Other names

abiraterone acetate + apalutamide