rucaparib + abiraterone

**Rucaparib + abiraterone** is an investigational oral combination therapy for prostate cancer, specifically metastatic castration-resistant prostate cancer (mCRPC)[2]. Rucaparib is a small molecule poly (ADP-ribose) polymerase (PARP) inhibitor that targets and inhibits PARP1, PARP2, and PARP3, essential enzymes in DNA repair. This action induces synthetic lethality in cancer cells with defects in homologous recombination repair, such as BRCA1/2 mutations[4][8]. Abiraterone is a small molecule inhibitor of the 17α-hydroxylase/C17,20-lyase (CYP17) enzyme, crucial for androgen biosynthesis. By inhibiting CYP17, abiraterone blocks androgen production, which is a key growth driver in prostate cancer[2][6]. The combination is designed to exploit vulnerabilities in prostate tumors that are androgen-driven and deficient in DNA repair mechanisms, aiming to improve outcomes by dual blockade of androgen synthesis and DNA damage repair[2]. This regimen is generally administered with prednisone to mitigate mineralocorticoid excess caused by CYP17 inhibition[2]. The combination remains investigational, with published clinical protocols exploring safety and efficacy in advanced prostate cancer patients[2].

Other names

rucaparibabiraterone acetate