Products
Rucaparib was approved in tablet form in the United States in 2016, in the EU in 2018, and in many countries in 2020 (Rubraca).
Structure and properties
Rucaparib (C19H18FN3O, Mr = 323.4 g/mol) is present in the drug as rucaparibcamsylate, a white to slightly yellow powder.
Effects
Rucaparib has antitumor and cytotoxic properties. The effects are due to inhibition of PARP (polyadenosine 5′-diphosphoribose polymerase) enzymes, which play an important role in DNA repair. The inhibition damages DNA and induces cell death. Rucaparib has a half-life between 17 to 19 hours.
Indications
For the treatment of advanced ovarian cancer with the -mutation.
Dosage
According to the SmPC. Tablets are taken twice daily, independent of meals.
Contraindications
Rucaparib is contraindicated in case of hypersensitivity. For complete precautions, see the drug label.
Interactions
Rucaparib is metabolized primarily by CYP2D6 and to a lesser extent by CYP1A2 and CYP3A4. It is a substrate of P-glycoprotein and BCRP.
Adverse effects
The most common potential adverse effects include nausea, fatigue, weakness, vomiting, anemia, abdominal pain, taste disturbances, constipation, poor appetite, diarrhea, thrombocytopenia, and respiratory disturbances.
