Olaparib

What it is and how it works

Mechanism of Action Olaparib is an inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, including PARP1, PARP2, and PARP3. PARP enzymes are involved in normal cellular functions, such as DNA transcription and DNA repair. Olaparib has been shown to inhibit growth of select tumor cell lines in vitro and decrease tumor growth in mouse xenograft models of human cancer, both as monotherapy or following platinum-based chemotherapy.

Mechanism class: Poly(ADP-Ribose) Polymerase Inhibitors

Indications

Lynparza is a poly (ADP-ribose) polymerase (PARP) inhibitor indicated: Ovarian cancer • for the maintenance treatment of adult patients with deleterious or suspected deleterious germline or somatic BRCA -mutated advanced epithelial ovarian, fallopian tube or primary peritoneal cancer who are in complete or partial response to first-line platinum-based chemotherapy. Select patients for therapy based on an FDA-approved companion diagnostic for Lynparza. ( 1.1 , 2.1 ) • in combination with bevacizumab for the maintenance treatment of adult patients with advanced epithelial ovarian, fallopian tube or primary peritoneal cancer who are in complete or partial response to first-line platinum-based chemotherapy and whose cancer is associated with homologous recombination deficiency (HRD)-positive status defined by either: • a deleterious or suspected deleterious BRCA mutation, and/or • genomic instability. Select patients for therapy based on an FDA-approved companion diagnostic for Lynparza.

Dosage and administration (summary)

• Recommended dosage is 300 mg taken orally twice daily with or without food. See Full Prescribing Information for the recommended duration. • Patients receiving Lynparza for mCRPC should also receive a gonadotropin-releasing hormone (GnRH) analog concurrently or should have had bilateral orchiectomy. • For moderate renal impairment (CLcr 31-50 mL/min), reduce Lynparza dosage to 200 mg orally twice daily. Patient Selection Information on FDA-approved tests for the detection of genetic mutations is available at http://www.fda.gov/companiondiagnostics .

Contraindications

None. None.

Warnings and precautions

• Myelodysplastic Syndrome/Acute Myeloid Leukemia (MDS/AML): Occurred in approximately 1.2% of patients with various BRCA m, g BRCA m, HRR gene-mutated or HRD-positive cancers exposed to Lynparza and the majority of events had a fatal outcome. Monitor patients for hematological toxicity at baseline and monthly thereafter. Discontinue if MDS/AML is confirmed. • Pneumonitis: Occurred in 1.0% of patients exposed to Lynparza, and some cases were fatal. Interrupt treatment if pneumonitis is suspected. Discontinue if pneumonitis is confirmed.

Pregnancy

Pregnancy Risk Summary Based on findings in animals and its mechanism of action , Lynparza can cause fetal harm when administered to a pregnant woman. There are no available data on Lynparza use in pregnant women to inform the drug-associated risk.

Storage and supply

Lynparza is available as 150 mg and 100 mg tablets. • 150 mg tablets: green to green/grey, oval, bi-convex, film-coated tablet, with debossment ‘OP150’ on one side and plain on the reverse, are available in: ∘ Bottles of 60 tablets (NDC 0310-0679-60) and ∘ Bottles of 120 tablets (NDC 0310-0679-12).

Source: Olaparib (Lynparza) — US FDA prescribing information, 2025-07-10, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.