Information about Rucaparib
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.
Liver safety of Rucaparib
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.
Mechanism of action of Rucaparib
Rucaparib (roo kap' a rib) is an orally available, small molecule inhibitor of poly adenine diphosphate (ADP)-ribose polymerase (PARP), an enzyme involved in DNA transcription and repair. Patients with mutations of the BRCA 1 and 2 genes are at increased risk for cancer, particularly ovarian and breast cancer in women. The BRCA gene encodes DNA repair enzymes, and tumor cells with BRCA mutations are dependent upon other pathways of DNA repair and thus have increased sensitivity to inhibition of PARP. Clinical trials of rucaparib in women with BRCA 1 and 2 germline mutations and advanced, refractory ovarian carcinoma have shown response rates of 30% to 40% and prolongation of progression free survival. Rucaparib is also under evaluation as therapy for advanced breast cancer and other malignant diseases associated mutations in BRCA or other DNA repair enzymes.
FDA approval information for Rucaparib
Rucaparib received approval for use in the United States in 2016 for therapy of advanced and refractory ovarian carcinoma in women with deleterious BRAC mutations.
Dosage and administration for Rucaparib
Rucaparib is available in 200 and 300 mg tablets under the brand name Rubraca. The recommended dose is 600 mg by mouth twice daily continued until disease progression or unacceptable toxicity occurs.
Side effects of Rucaparib
Common side effects include anemia, fatigue, nausea, diarrhea, constipation, dyspepsia, abdominal pain, anorexia, shortness of breath and thrombocytopenia. Uncommon, but potentially severe side effects include myelodysplastic syndrome and embryo-fetal toxicity.