Comprehensive Guide to Olaparib: Uses, Dosage, Side Effects, and More
What is Olaparib?
Overview of Olaparib
Generic Name: Olaparib
Brand Name: Lynparza, generics
Drug Group: PARP inhibitor (antineoplastic)
Commonly Used For
- Treat ovarian cancer.
- Manage breast cancer.
- Control prostate cancer.
Key Characteristics
Form: Oral tablets (100 mg, 150 mg) or capsules (50 mg) (detailed in Dosage section).
Mechanism: Inhibits PARP enzymes, inducing synthetic lethality in BRCA-mutated cells.
Approval: FDA-approved (2014 for Lynparza) and EMA-approved for multiple cancers.
Indications and Uses of Olaparib
Olaparib is indicated for various cancers with DNA repair deficiencies, leveraging its targeted mechanism:
Ovarian Cancer (BRCA-Mutated): Treats advanced ovarian cancer in patients with germline or somatic BRCA1/2 mutations, as maintenance therapy post-chemotherapy, improving progression-free survival, per oncology guidelines.
Breast Cancer (HER2-Negative, BRCA-Mutated): Manages metastatic breast cancer in patients with BRCA1/2 mutations, enhancing response rates, supported by clinical trials like OlympiAD.
Prostate Cancer (BRCA-Mutated, Metastatic): Treats metastatic castration-resistant prostate cancer (mCRPC) with BRCA1/2 or other HRR mutations, delaying disease progression, per urologic oncology data.
Pancreatic Cancer (BRCA-Mutated): Used for maintenance in metastatic pancreatic cancer with BRCA mutations, improving outcomes, supported by POLO trial results.
Endometrial Cancer: Investigated off-label for endometrial cancer with DNA repair defects, reducing tumor growth, with emerging gynecologic oncology evidence.
Fallopian Tube Cancer: Employed off-label for BRCA-mutated fallopian tube cancer, enhancing control, supported by gynecologic studies.
Primary Peritoneal Cancer: Managed off-label in BRCA-mutated primary peritoneal cancer, improving survival, with data from oncology cohorts.
Small Cell Lung Cancer (SCLC): Explored off-label for SCLC with HRR mutations, enhancing sensitivity to chemotherapy, with pulmonary oncology research.
Glioblastoma: Investigated off-label for glioblastoma with DNA repair deficiencies, improving response in combination therapy, noted in neuro-oncology trials.
Triple-Negative Breast Cancer (TNBC): Used off-label in TNBC with BRCA-like features, reducing recurrence, supported by breast cancer research.
Dosage of Olaparib
Dosage for Adults
Ovarian Cancer (Maintenance): 300 mg twice daily (two 150 mg tablets), taken with or without food.
Breast Cancer (HER2-Negative, BRCA-Mutated): 300 mg twice daily, continued until disease progression.
Prostate Cancer (mCRPC): 300 mg twice daily, with or without food, in combination with androgen deprivation therapy.
Pancreatic Cancer (Maintenance): 300 mg twice daily, adjusted for toxicity.
Dosage for Children
Not Approved: Not recommended for pediatric use due to limited data; consult a pediatric oncologist for off-label consideration.
Dosage for Pregnant Women
Pregnancy Category D: Avoid unless benefits outweigh risks (e.g., life-threatening cancer). Consult an obstetrician, with fetal monitoring.
Dosage Adjustments
Renal Impairment: No adjustment needed; monitor if CrCl 30–50 mL/min; avoid if <30 mL/min.
Hepatic Impairment: No adjustment needed; monitor in moderate (Child-Pugh B) cases; avoid severe (Child-Pugh C).
Myelosuppression: Reduce to 250 mg twice daily if grade 3/4 neutropenia or anemia occurs; discontinue if persistent.
Elderly: Start with 250 mg twice daily; increase to 300 mg if tolerated.
Concomitant Medications: Avoid CYP3A inhibitors/inducers (e.g., itraconazole, rifampin); adjust dose if unavoidable.
Additional Considerations
- Take this active ingredient with or without food, using a glass of water.
- Swallow tablets whole; do not crush or chew.
How to Use Olaparib
Administration:
- Swallow tablets whole with water, with or without food; avoid grapefruit juice.
- Take at the same time daily (e.g., morning and evening) for consistency.
Timing: Use twice daily, maintaining a 12-hour interval.
Monitoring: Watch for fatigue, bruising, or signs of infection (e.g., fever).
Additional Tips:
- Store at 20–25°C (68–77°F), protecting from moisture and heat.
- Keep out of reach of children due to toxicity risk.
- Report severe abdominal pain, shortness of breath, or signs of allergic reaction immediately.
Contraindications for Olaparib
Hypersensitivity: Patients with a known allergy to Olaparib or PARP inhibitors.
Severe Renal/Hepatic Impairment: Avoid if CrCl <30 mL/min or Child-Pugh C.
Pregnancy: Contraindicated unless life-saving.
Side Effects of Olaparib
Common Side Effects
- Nausea (60–70%, managed with antiemetics)
- Fatigue (50–65%, decreases with rest)
- Anemia (30–50%, monitored with blood tests)
- Vomiting (25–40%, reduced with hydration)
- Diarrhea (20–35%, transient)
These effects may subside with dose adjustment.
Serious Side Effects
Seek immediate medical attention for:
- Hematologic: Neutropenia, thrombocytopenia, or severe anemia.
- Pulmonary: Interstitial lung disease or pneumonitis.
- Hepatic: Elevated liver enzymes or jaundice.
- Oncologic: Myelodysplastic syndromes (MDS) or acute myeloid leukemia (AML).
- Allergic: Rash, angioedema, or anaphylaxis.
Additional Notes
- Regular monitoring for blood counts, liver function, and lung health is advised.
- Report any unusual symptoms (e.g., fever, persistent cough) immediately to a healthcare provider.
Warnings & Precautions for Olaparib
General Warnings
Myelosuppression: Risk of neutropenia, anemia, and thrombocytopenia; monitor blood counts every month.
Pneumonitis: Rare interstitial lung disease; assess respiratory symptoms.
Secondary Malignancies: Increased risk of MDS/AML; screen regularly.
Embryofetal Toxicity: Severe risk; use effective contraception.
Gastrointestinal Toxicity: Nausea and vomiting; use antiemetics.
Additional Warnings
Venous Thromboembolism: Risk of DVT/PE; monitor for leg pain or swelling.
Cardiotoxicity: Rare QT prolongation; assess ECG in at-risk patients.
Infections: Higher risk due to immunosuppression; prophylaxis may be needed.
Renal Impairment: Monitor kidney function; adjust if needed.
Hypersensitivity Reactions: Rare anaphylaxis; discontinue if swelling occurs.
Use in Specific Populations
- Pregnancy: Category D; avoid unless critical; use contraception.
- Breastfeeding: Avoid due to potential toxicity; monitor infant.
- Elderly: Higher risk of myelosuppression; start with lower doses.
- Children: Not approved; use only off-label with caution.
- Renal/Hepatic Impairment: Adjust dose; avoid in severe cases.
Additional Precautions
- Inform your doctor about kidney/liver disease, prior cancers, or medication history before starting this medication.
- Avoid abrupt cessation; taper if combined with other therapies.
Overdose and Management of Olaparib
Overdose Symptoms
- Nausea, vomiting, or severe fatigue.
- Severe cases: Myelosuppression, liver damage, or pneumonitis.
- Dizziness, bruising, or shortness of breath as early signs.
- Seizures with extremely high doses.
Immediate Actions
Contact the Medical Team: Seek immediate medical help.
Supportive Care: Administer IV fluids, blood transfusions, and oxygen if needed.
Specific Treatment: No antidote; manage symptoms and monitor organ function.
Monitor: Check blood counts, liver enzymes, and respiratory status for 7–14 days.
Additional Notes
- Overdose risk is low; store securely.
- Report persistent symptoms (e.g., jaundice, severe weakness) promptly.
Drug Interactions with Olaparib
This active ingredient may interact with:
- CYP3A Inhibitors: Increases levels (e.g., ketoconazole); reduce dose to 150 mg twice daily.
- CYP3A Inducers: Decreases levels (e.g., rifampin); avoid or increase dose cautiously.
- Anticoagulants: Alters bleeding risk (e.g., warfarin); monitor INR.
- Statins: Enhances myopathy risk (e.g., simvastatin); use alternatives.
- Antiepileptics: Alters metabolism (e.g., phenytoin); adjust dose.
Action: Provide your healthcare provider with a complete list of medications.
Patient Education or Lifestyle
Medication Adherence: Take this PARP inhibitor as prescribed in cancer therapy, following the exact schedule.
Monitoring: Report bruising, fatigue, or respiratory issues immediately.
Lifestyle: Avoid smoking; maintain a nutrient-rich diet.
Diet: Take with or without food; avoid grapefruit to prevent interactions.
Emergency Awareness: Know signs of infection, lung issues, or bleeding; seek care if present.
Follow-Up: Schedule regular check-ups every 1–3 months to monitor blood, liver, and cancer progression.
Pharmacokinetics of Olaparib
Absorption: Well-absorbed orally (peak at 1–3 hours); unaffected by food but avoid inhibitors.
Distribution: Volume of distribution ~167 L; 82% protein-bound.
Metabolism: Hepatic via CYP3A4 and CYP2D6 to inactive metabolites.
Excretion: Primarily renal (44%) and fecal (42%) as metabolites; half-life 11.9 hours.
Half-Life: 11.9 hours, with sustained PARP inhibition.
Pharmacodynamics of Olaparib
This drug exerts its effects by:
- Inhibiting PARP1 and PARP2, preventing DNA single-strand break repair in BRCA-mutated cells.
- Inducing synthetic lethality, selectively killing cancer cells with HRR deficiencies.
- Enhancing chemotherapy/radiotherapy efficacy in combination settings.
- Exhibiting dose-dependent myelosuppression and gastrointestinal toxicity.
Storage of Olaparib
Temperature: Store at 20–25°C (68–77°F); protect from moisture.
Protection: Keep in original container, away from light.
Safety: Store in a locked container out of reach of children due to toxicity risk.
Disposal: Dispose of unused tablets per local regulations or consult a pharmacist.
Frequently Asked Questions (FAQs)
Q: What does Olaparib treat?
A: This medication treats ovarian, breast, and prostate cancers.
Q: Can this active ingredient cause fatigue?
A: Yes, fatigue may occur; rest and report if severe.
Q: Is Olaparib safe for children?
A: No, not approved; consult a doctor for off-label use.
Q: How is this drug taken?
A: Orally as tablets twice daily, as directed.
Q: How long is Olaparib treatment?
A: Varies by cancer type, often until progression.
Q: Can I use Olaparib if pregnant?
A: No, avoid unless life-saving; consult a doctor.
Regulatory Information
This medication is approved by:
U.S. Food and Drug Administration (FDA): Approved in 2014 (Lynparza) for ovarian cancer, expanded to breast, prostate, and pancreatic cancers.
European Medicines Agency (EMA): Approved for multiple cancer indications.
Other Agencies: Approved globally for oncology; consult local guidelines.
References
- U.S. Food and Drug Administration (FDA). (2025). Lynparza (Olaparib) Prescribing Information.
- Official FDA documentation detailing the drug’s approved uses, dosage, and safety.
- European Medicines Agency (EMA). (2025). Olaparib Summary of Product Characteristics.
- EMA’s comprehensive information on the medication’s indications and precautions in Europe.
- National Institutes of Health (NIH). (2025). Olaparib: MedlinePlus Drug Information.
- NIH resource providing detailed information on the drug’s uses, side effects, and precautions.
- World Health Organization (WHO). (2025). WHO Guidelines on Cancer Therapy: Olaparib.
- WHO’s recommendations for Olaparib in cancer management.
- New England Journal of Medicine. (2024). Olaparib in BRCA-Mutated Cancers.
- Peer-reviewed article on Olaparib efficacy (note: access may require a subscription).
