Rucaparib is a PARP inhibitor used as an anti-cancer agent. Rucaparib is a first-in-class pharmaceutical drug targeting the DNA repair enzyme poly-ADP ribose polymerase-1 (PARP-1). It was discovered as part of a collaboration between scientists Rucaparib is in clinical development for the treatment of metastatic castration-resistant prostate cancer (mCRPC) patients in the TRITON2 trial for patients with BRCA mutations (inclusive of germline and somatic) and also enrolling patients with deleterious mutations of other HR repair genes, including ATM, and the TRITON3 trial for patients with BRCA mutations and ATM mutations who have progressed on AR-targeted therapy and who have not yet received chemo in the castrate-resistant setting. Both trials are open for enrollment.
Rucaparib is a small molecule inhibitor of poly ADP-ribose polymerase that is used in the therapy of selected patients with refractory and advanced ovarian carcinoma. Rucaparib therapy is associated with a moderate rate of transient elevations in serum aminotransferase during therapy, but has not been linked to instances of clinically apparent liver injury.