Rucaparib (RUBRACAⓇ) is the first FDA-approved poly (ADP-ribose) polymerase (PARP) inhibitor for men with BRCA mutation-associated metastatic castration-resistant prostate cancer (mCRPC). Rucaparib's efficacy in patients with mCRPC associated with DNA damage repair (DDR) deficiency was demonstrated in the TRITON2 and TRITON3 trials. In TRITON2, rucaparib demonstrated meaningful antitumor activity in men with measurable BRCA-mutated disease, with objective responses observed across both germline and somatic mutations. In TRITON3, rucaparib improved radiographic progression-free survival (rPFS) over physician's choice of therapy (docetaxel or a second-generation androgen-receptor pathway inhibitor [ARPI]). Rucaparib is the only drug to have shown improved rPFS versus docetaxel in mCRPC. Rucaparib demonstrated a consistent and manageable safety profile similar to other PARP inhibitors, with the most common adverse events being fatigue/asthenia, musculoskeletal pain, nausea, and anemia/decreased hemoglobin. Men with mCRPC face prolonged and complex treatments, during which maintaining quality of life, minimizing toxicity, and preserving functional status are major priorities. For patients with BRCA mutations, rucaparib offers a targeted oral alternative to chemotherapy that can delay mCRPC progression while reducing many of the logistical, physical, and clinical burdens commonly associated with chemotherapy. Its oral administration and flexible dosing enable an individualized approach that reduces treatment interruptions and maximizes clinical benefits.
Rucaparib is a tablet used to treat advanced prostate cancer that has spread and no longer responds to standard hormone treatment (metastatic castration-resistant prostate cancer; mCRPC). It is used in patients whose cancer has certain gene variations, such as BRCA1 or BRCA2, which affect how cancer cells repair damage. It is taken twice a day with or without food. It comes in different strengths, which allows doctors to adjust the dose if needed. In clinical studies, rucaparib helped slow the growth of cancer in men with this type of prostate cancer. In the TRITON3 trial, patients taking rucaparib lived longer without their cancer getting worse or spreading (also called progression-free survival; PFS) compared with those on other common treatments (chemotherapy or second-generation androgen-receptor pathway inhibitors). Rucaparib is the only treatment shown to control cancer growth longer than chemotherapy in patients with mCRPC. The side effects of rucaparib are manageable with close monitoring. The most common side effects include fatigue, body pain, nausea, and low red blood cells, which are similar to other drugs of its kind and can be managed with supportive care and reducing the dose. Additionally, rucaparib’s safety profile is similar in patients across age groups, including those that are 75 years and older. Rucaparib offers an oral, targeted alternative to chemotherapy that can delay cancer progression while helping patients avoid frequent clinic visits, disruptions to daily life, and unwanted side effects. Based on the clinical evidence, rucaparib is a beneficial treatment option for patients with BRCA-mutated mCRPC.
Future oncology (London, England). 2026 Jun 18 [Epub ahead of print]
Alan Haruo Bryce, Paige Nash, Anne Roessler, Divneet Mandair
Department of Medical Oncology & Therapeutics Research, City of Hope Cancer Center Phoenix, Goodyear, AZ, USA., Pharmacy Department, City of Hope Cancer Center Phoenix, Goodyear, AZ, USA., Medical Affairs, Tolmar, Inc., Buffalo Grove, IL, USA.