Products
Olaparib was approved in the United States and EU in 2014 and in many countries in 2015 in capsule form (Lynparza). Later, film-coated tablets were also registered.
Structure and properties
Olaparib (C24H23FN4O3, Mr = 434.5 g/mol)
Effects
Olaparib (ATC L01XX46) has antitumor and cytotoxic properties. The effects are due to inhibition of PARP (poly-(ADP-ribose) polymerase) enzymes. These enzymes are involved in DNA transcription, cell cycle regulation, and DNA repair. The half-life is approximately 12 hours.
Indications
For maintenance therapy in patients with advanced, recurrent ovarian cancer with the BRCA mutation. Following platinum-containing chemotherapy in the presence of complete or partial remission.
Dosage
According to the SmPC. Capsules are taken twice daily (morning and evening). They are taken fasting, at least one hour after a meal. Subsequently, no food should be eaten for two hours.
Contraindications
- Hypersensitivity
- Pregnancy
- Lactation
Full precautions can be found in the drug label.
Interactions
Olaparib is metabolized primarily by CYP3A and is a substrate of P-glycoprotein. Corresponding drug-drug interactions are possible. Combination with cytostatic agents increases the risk for adverse reactions.
Adverse effects
The most common possible adverse effects include nausea, vomiting, diarrhea, dyspepsia, fatigue, headache, taste disturbances, decreased appetite, dizziness, anemia, neutropenia, lymphopenia, an increase in mean corpuscular volume, and an increase in creatinine.
