Products
Talazoparib is commercially available in hard capsule form (Talzenna). It was approved in the United States in 2018 and in the EU and many countries in 2019.
Structure and properties
Talazoparib exists in the drug as talazoparib tosilate, a white to yellow solid. Fluorination of the drug prevents oxidative metabolism.
Effects
Talazoparib (ATC L01XX60) has antitumor, cytotoxic, and antiproliferative properties. The effects are due to inhibition of the PARP enzymes PARP-1 and PARP-2, which are involved in DNA repair, gene transcription, and cell death, for example. Enzyme inhibition leads to cell death of cancer cells. The half-life is approximately 90 hours.
Indications
For the treatment of adult patients with germline BRCA1/2 mutations who have HER2-negative, locally advanced, or metastatic breast carcinoma (breast cancer).
Dosage
According to the SmPC. Capsules are taken once daily, independent of meals.
Contraindications
- Hypersensitivity
- Breastfeeding
Full precautions can be found in the drug label.
Interactions
Talazoparib is a substrate of P-glycoprotein and BCRP. It is poorly metabolized and eliminated mainly unchanged by the kidneys. Talazoparib does not interact with CYP450 isozymes.
Adverse effects
The most common potential adverse effects include:
- Fatigue, headache
- Nausea
- Anemia, neutropenia, thrombocytopenia
