Olaparib

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.

• 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.ICD-10: C56.9

• None. None.contraindicated

• Recommended dosage is 300 mg taken orally twice daily with or without food. See Full Prescribing Information for the recommended duration. (2.2) • Patients receiving Lynparza for mCRPC should also receive a gonadotropin-releasing hormone (GnRH) analog concurrently or should have had bilateral orchiectomy. (2.2) • For moderate renal impairment (CLcr 31-50 mL/min), reduce Lynparza dosage to 200 mg orally twice daily. (2.5) 2.1 Patient Selection Information on FDA-approved tests for the detection of genetic mutations is available at http://www.fda.gov/companiondiagnostics . Select patients for treatment with Lynparza based on the presence of deleterious or suspected deleterious HRR gene mutations, including BRCA mutations, or genomic instability based on the indication, biomarker, and sample type (Table 1). Table 1 Biomarker Testing for Patient Selection Where testing fails or tissue sample is unavailable/insufficient, or when germline testing is negative, consider using an alternative test, if available.

• 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. (5.1) • 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. (5.2) • Venous thromboembolism (VTE), including severe or fatal pulmonary embolism (PE), occurred in patients treated with Lynparza. VTE occurred in 8% of patients with mCRPC. Monitor patients for signs and symptoms of VTE and PE and treat as medically appropriate. ( 5.3 ) • Hepatotoxicity, Including Drug-induced liver injury (DILI): Occurred in patients treated with Lynparza. If DILI is suspected, interrupt Lynparza. If DILI is confirmed, discontinue treatment. ( 5.4 ) • Embryo-Fetal Toxicity: Can cause fetal harm. Advise of the potential risk to a fetus and to use effective contraception. ( 5.5 , 8.1 , 8.3 ) 5.1 Myelodysplastic Syndrome/Acute Myeloid Leukemia Myelodysplastic syndrome (MDS)/Acute Myeloid Leukemia (AML) has occurred in patients treated with Lynparza and some cases were fatal.

The following adverse reactions are discussed elsewhere in the labeling: • Myelodysplastic Syndrome/Acute Myeloid Leukemia [see Warnings and Precautions (5.1) ] • Pneumonitis [see Warnings and Precautions (5.2) ] • Venous Thromboembolism [see Warnings and Precautions (5.3) ] • Hepatotoxicity, Including Drug-Induced Liver Injury [see Warnings and Precautions (5.4) ] Most common adverse reactions (≥10%): • as a single agent were nausea, fatigue (including asthenia), anemia, vomiting, diarrhea, decreased appetite, headache, dysgeusia, cough, neutropenia, dyspnea, dizziness, dyspepsia, leukopenia, and thrombocytopenia. (6.1) • in combination with bevacizumab were nausea, fatigue (including asthenia), anemia, lymphopenia, vomiting, diarrhea, neutropenia, leukopenia, urinary tract infection, and headache. ( 6.1 ) • in combination with abiraterone and prednisone or prednisolone were anemia, fatigue, nausea, diarrhea, decreased appetite, lymphopenia, dizziness, and abdominal pain. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact AstraZeneca at 1-800-236-9933 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trial Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

Lactation: Advise women not to breastfeed. (8.2) 8.1 Pregnancy Risk Summary Based on findings in animals and its mechanism of action [see Clinical Pharmacology (12.1) ] , 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. In an animal reproduction study, the administration of olaparib to pregnant rats during the period of organogenesis caused teratogenicity and embryo-fetal toxicity at exposures below those in patients receiving the recommended human dose of 300 mg twice daily (see Data ). Apprise pregnant women of the potential hazard to the fetus and the potential risk for loss of the pregnancy. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. The estimated background risk in the U.S. general population of major birth defects is 2-4%; and the risk for spontaneous abortion is approximately 15-20% in clinically recognized pregnancies. Data Animal Data In a fertility and early embryonic development study in female rats, olaparib was administered orally for 14 days before mating through to Day 6 of pregnancy, which resulted in increased post-implantation loss at a dose level of 15 mg/kg/day (with maternal systemic exposures approximately 7% of the human exposure (AUC 0-24h ) at the recommended dose).

Metabolism

The area under the curve (AUC) of olaparib increases approximately proportionally following administration of single doses of 25 mg to 450 mg (0.08 to 1.5 times the recommended dose) and maximal concentrations (C max ) increased slightly less than proportionally for the same dose range. Olaparib showed time-dependent pharmacokinetics and an AUC mean accumulation ratio of 1.8 is observed at steady state following a dose of 300 mg twice daily.

• Aug 17, 2017NDANDA208558Astrazeneca

1. 1Death4,62923%
2. 2Malignant Neoplasm Progression2,00810.0%
3. 3Nausea1,7558.7%
4. 4Fatigue1,6678.3%
5. 5Anaemia1,5697.8%
6. 6Off Label Use9044.5%
7. 7Vomiting7043.5%
8. 8Drug Ineffective6633.3%
9. 9Diarrhoea6003.0%
10. 10Asthenia5752.9%
11. 11Neuropathy Peripheral5702.8%
12. 12Decreased Appetite5262.6%
13. 13Disease Progression4922.4%
14. 14Myelodysplastic Syndrome4722.3%
15. 15Haemoglobin Decreased4252.1%

The 10 most recently updated of 497 ClinicalTrials.gov registrations naming Olaparib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Roll Over StudY for Patients Who Have Completed a Previous Oncology Study With Olaparib
  Active not recruiting · Phase 3 · Interventional · 185 enrolled · AstraZeneca
  NCT04421963updated 2026-06-12
• Targeted Therapy Directed by Genetic Testing in Treating Patients With Locally Advanced or Advanced Solid Tumors, The ComboMATCH Screening Trial
  Recruiting · Phase 2 · Interventional · 2,900 enrolled · National Cancer Institute (NCI)
  NCT05564377updated 2026-06-12
• Long-term Safety and Efficacy Extension Study for Participants With Advanced Tumors Who Are Currently on Treatment or in Follow-up in a Pembrolizumab (MK-3475) Study (MK-3475-587/KEYNOTE-587)
  Recruiting · Phase 3 · Interventional · 3,500 enrolled · Merck Sharp & Dohme LLC
  NCT03486873updated 2026-06-12
• mTORC1/2 Inhibitor AZD2014 or the Oral AKT Inhibitor AZD5363 for Recurrent Endometrial and Ovarian
  Active not recruiting · Phase 1 · Interventional · 159 enrolled · M.D. Anderson Cancer Center
  NCT02208375updated 2026-06-12
• A Clinical Study of Sacituzumab Tirumotecan (Sac-TMT, MK-2870) in People With Breast Cancer (MK-2870-032)
  Recruiting · Phase 3 · Interventional · 2,400 enrolled · Merck Sharp & Dohme LLC
  NCT06966700updated 2026-06-12
• Olaparib and Durvalumab With Carboplatin, Etoposide, and/or Radiation Therapy for the Treatment of Extensive-Stage Small Cell Lung Cancer, PRIO Trial
  Active not recruiting · Phase 1 · Phase 2 · Interventional · 63 enrolled · M.D. Anderson Cancer Center
  NCT04728230updated 2026-06-11
• A Study of BL-B01D1 Combination Therapy in Patients With Metastatic Castration-resistant Prostate Cancer
  Not yet recruiting · Phase 2 · Phase 3 · Interventional · 180 enrolled · Sichuan Baili Pharmaceutical Co., Ltd.
  NCT07641855updated 2026-06-11
• Testing the Safety of Different Doses of Olaparib Given Radium-223 for Men With Advanced Prostate Cancer With Bone Metastasis
  Active not recruiting · Phase 1 · Phase 2 · Interventional · 132 enrolled · National Cancer Institute (NCI)
  NCT03317392updated 2026-06-11
• Testing Olaparib in Patients With Advanced or Metastatic (Cancer That Has Spread) Bladder Cancer and Other Genitourinary Tumors With DNA-Repair Genetic Changes
  Active not recruiting · Phase 2 · Interventional · 60 enrolled · National Cancer Institute (NCI)
  NCT03375307updated 2026-06-11
• APOLLO: A Randomized Phase II Double-Blind Study of Olaparib Versus Placebo Following Curative Intent Therapy in Patients With Resected Pancreatic Cancer and a Pathogenic BRCA1, BRCA2 or PALB2 Mutation
  Recruiting · Phase 2 · Interventional · 152 enrolled · National Cancer Institute (NCI)
  NCT04858334updated 2026-06-11

Frequently asked questions

How does Olaparib work?

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.

What is Olaparib used for?

According to FDA labeling, Olaparib carries indications including: 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.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Olaparib?

Olaparib is classified as Poly (ADP-ribose) polymerase (PARP) inhibitors, Poly(ADP-Ribose) Polymerase Inhibitor, Poly(ADP-Ribose) Polymerase Inhibitors, Cellular Growth Phase Reduction, Decreased DNA Integrity, Decreased Reverse Transcription to DNA.

What are the brand names for Olaparib?

Olaparib is marketed under brand names including Lynparza.

What are the contraindications for Olaparib?

Olaparib labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.