Niraparib

Products

Niraparib was approved in the US and EU in 2017 and in many countries in 2018 in hard capsule form (Zejula).

Structure and properties

Niraparib (C19H20N4O, Mr = 320.4 g/mol) is present in the drug as niraparibtosilate monohydrate. It is a piperidine, indazole, and carboxamide derivative.

Effects

Niraparib (ATC L01XX54) has antitumor and cytotoxic properties. The effects are due to inhibition of PARP enzymes 1 and 2, which are important for DNA repair (PARP: poly-(ADP-ribose) polymerase). This leads to DNA damage and programmed cell death in the cell. The half-life is in the range of about two days.

Indications

For the treatment of serous ovarian carcinoma, carcinoma of the tubes, or in primary peritoneal carcinomatosis.

Dosage

According to the SmPC. Capsules are taken once daily, regardless of meals, and always at the same time of day.

Contraindications

  • Hypersensitivity
  • Breastfeeding

Full precautions can be found in the drug label.

Interactions

Niraparib is a substrate of carboxylesterases, UDP-glucuronosyl transferases, and P-glycoprotein and BCRP.

Adverse effects

The most common potential adverse effects include:

  • Fatigue, weakness, insomnia, headache, dizziness.
  • Nausea, constipation, vomiting, abdominal pain, taste disturbance, decreased appetite, diarrhea, dyspepsia,
  • Nasopharyngitis, dyspnea, cough.
  • Urinary tract infections
  • Hypertension, palpitations
  • Back pain, joint pain
  • Thrombocytopenia, neutropenia, anemia.