Olaparib

Generic Details

Generic Name

Olaparib

Other Names

  • Lynparza

Drug Class

  • Poly(ADP-ribose) polymerase (PARP) inhibitor

Chemical Formula

C24H23FN4O3

Molecular Weight

434.47 g/mol

Mechanism of Action

  • Inhibitor of poly ADP-ribose polymerase (PARP) enzymes, resulting in the trapping of PARP on DNA single-strand breaks, leading to cytotoxicity.

Indications

  • Ovarian cancer
  • Breast cancer
  • Pancreatic cancer
  • Prostate cancer

Common Dosage Forms

  • Tablet
  • Capsule

Typical Dosage

  • 300 mg twice daily

Pediatric Dosage

  • Safety and efficacy not established in pediatric patients.

Geriatric Dosage

  • Adjust dosage based on individual patient requirements and renal function.

Side Effects

  • Nausea
  • Fatigue
  • Anemia
  • Vomiting
  • Diarrhea
  • Headache

Contraindications

  • Hypersensitivity to olaparib or any component of the formulation

Pregnancy Category

  • D - Use in pregnancy only if the potential benefit justifies the potential risk to the fetus.

Lactation Safety

  • Not recommended during breastfeeding.

Drug Interactions

  • Strong CYP3A4 and CYP2D6 inhibitors may increase olaparib concentrations

Overdose Symptoms

  • Increased risk of severe myelosuppression

Antidote for Overdose

  • No specific antidote, manage with supportive care and monitoring

Storage Conditions

  • Store at room temperature, protect from moisture and light

Pharmacokinetics

  • Absorption: Rapidly absorbed after oral administration
  • Distribution: Extensively distributed, primarily bound to plasma proteins
  • Metabolism: Primarily metabolized in the liver via CYP3A4 and CYP2D6 enzymes
  • Excretion: Mainly excreted in feces and urine

Precautions

  • Monitor blood counts regularly due to the risk of myelosuppression

Warnings

  • May cause myelodysplastic syndrome or acute myeloid leukemia
  • May increase the risk of developing secondary malignancies

Others

  • May cause pneumonitis, embryotoxic and teratogenic potential