Olaparib (olaparib)
Olaparib is a parp inhibitor (poly (adp-ribose) polymerase inhibitor) from AstraZeneca (distributed by AstraZeneca Pharmaceuticals LP); developed and commercialised in collaboration with Merck (MSD outside the US and Canada), marketed originally as Lynparza. This monograph covers approved indications, mechanism, dosing, side effects and the manufacturer landscape.
Overview
Olaparib (Lynparza) was the first oral poly (ADP-ribose) polymerase (PARP) inhibitor to reach the clinic and remains the broadest in its class, with approvals spanning ovarian, breast, pancreatic and prostate cancer. Its mechanism exploits synthetic lethality: PARP enzymes (PARP1, PARP2 and PARP3) are needed to repair single-strand DNA breaks, and cancer cells that already carry a defect in homologous recombination repair - most often a BRCA1 or BRCA2 mutation, but also other HRR gene mutations - cannot cope when PARP is blocked as well. The two unrepaired defects overwhelm the cell, which accumulates double-strand breaks and dies. The standard dose is 300 mg twice daily, given as two 150 mg tablets, with or without food, and continued until progression or unacceptable toxicity; first-line maintenance in BRCA-mutated advanced ovarian cancer is capped at two years. Olaparib is used as maintenance after platinum-based chemotherapy in newly diagnosed BRCA-mutated (or, with bevacizumab, HRD-positive) ovarian cancer; as maintenance in recurrent platinum-sensitive ovarian cancer; as treatment for germline BRCA-mutated advanced ovarian cancer after three or more prior lines; for gBRCAm HER2-negative metastatic breast cancer after chemotherapy; as maintenance for gBRCAm metastatic pancreatic cancer that has not progressed on at least 16 weeks of platinum therapy; and for homologous recombination repair (HRR)-mutated metastatic castration-resistant prostate cancer after enzalutamide or abiraterone. Nausea, fatigue, anaemia and abdominal pain dominate the side-effect profile; anaemia is grade 3-4 in about 21% of patients, so blood counts need monthly monitoring. Myelodysplastic syndrome and acute myeloid leukaemia are rare (under 1. 5%) but serious late complications. An important regulatory milestone is that Natco Pharma's generic olaparib tablets have received USFDA tentative approval, meaning the formulation met the regulatory requirements for bioequivalence against the reference product Lynparza.
How it works
Olaparib blocks PARP, an enzyme that cancer cells use to repair damaged DNA. Cancer cells that already have a faulty DNA-repair gene (such as BRCA1 or BRCA2) cannot fix the damage when PARP is also blocked, so they die. It is used mostly in cancers linked to BRCA mutations - ovarian, breast, pancreatic and prostate cancer.
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 tumour cell lines in vitro and decrease tumour growth in mouse xenograft models of human cancer, both as a single agent or in combination with established chemotherapies. (FDA label, section 12. 1)
Approved indications
- Maintenance treatment of adults with deleterious or suspected deleterious germline or somatic BRCA-mutated advanced epithelial ovarian, fallopian tube or primary peritoneal cancer in complete or partial response to first-line platinum-based chemotherapy
- In combination with bevacizumab, maintenance treatment of adults with advanced epithelial ovarian, fallopian tube or primary peritoneal cancer in complete or partial response to first-line platinum-based chemotherapy whose cancer is HRD-positive (BRCA mutation and/or genomic instability)
- Maintenance treatment of adults with recurrent epithelial ovarian, fallopian tube or primary peritoneal cancer in complete or partial response to platinum-based chemotherapy
- Treatment of adults with deleterious or suspected deleterious germline BRCA-mutated advanced ovarian cancer who have been treated with three or more prior lines of chemotherapy
- Treatment of adults with deleterious or suspected deleterious gBRCAm, HER2-negative metastatic breast cancer who have been treated with chemotherapy in the neoadjuvant, adjuvant or metastatic setting
- Maintenance treatment of adults with deleterious or suspected deleterious gBRCAm metastatic pancreatic adenocarcinoma whose disease has not progressed on at least 16 weeks of first-line platinum-based chemotherapy
- Treatment of adults with deleterious or suspected deleterious germline or somatic homologous recombination repair (HRR) gene-mutated metastatic castration-resistant prostate cancer (mCRPC) who have progressed following prior treatment with enzalutamide or abiraterone (FDA approval, May 19, 2020)
Dosage & administration
300 mg (two 150 mg tablets) taken orally twice daily, with or without food (total daily dose 600 mg). Continue until disease progression or unacceptable toxicity; for first-line maintenance of BRCA-mutated advanced ovarian cancer, continue until progression, unacceptable toxicity, or completion of 2 years of treatment.
Dose adjustment
For adverse reactions, first dose reduction is 250 mg twice daily; a further reduction is 200 mg twice daily. With a strong CYP3A inhibitor that cannot be avoided, reduce to 100 mg twice daily; with a moderate CYP3A inhibitor, reduce to 150 mg twice daily. Moderate renal impairment (CLcr 31-50 mL/min): reduce to 200 mg twice daily.
Side effects
Nausea (77%) · Fatigue / asthenia (67%) · Anemia (38%; Grade 3-4 in 21%) · Abdominal pain (45%) · Vomiting (40%) · Diarrhea (37%) · Constipation (28%) · Dysgeusia (26%) · Dizziness (20%) · Decreased appetite (20%) · Neutropenia (17%) · Leukopenia (13%) · Dyspnea (15%) · Upper respiratory tract infection / nasopharyngitis (28%)
- Thrombocytopenia (11%)
- Myelodysplastic syndrome / acute myeloid leukemia (MDS/AML, <1. 5%)
- Pneumonitis (<1%)
Monitoring
- Complete blood count for cytopenia at baseline and monthly thereafter for clinically significant changes during treatment (monitor for MDS/AML)
- For prolonged haematological toxicity, interrupt treatment and monitor blood counts weekly until recovery; if not recovered to Grade 1 or less after 4 weeks, refer to a haematologist including bone marrow analysis
- Monitoring for new or worsening respiratory symptoms (dyspnea, cough, fever) or radiological abnormality that could indicate pneumonitis
- Do not start until patients have recovered from haematological toxicity caused by previous chemotherapy (<=Grade 1)
Generic and biosimilar landscape
Natco Pharma's generic olaparib tablets (100 mg and 150 mg) received USFDA tentative approval, meaning the formulation met the regulatory requirements for bioequivalence, safety, efficacy and quality against the reference listed drug Lynparza. Bangladeshi olaparib products (Beacon Olapar, Incepta Olacent, Everest Olanib) are DGDA-registered and made under the TRIPS least-developed-country patent exemption, not as FDA/EMA-approved generics; no published BE study against Lynparza was found for them.
Who makes it
| Manufacturer | Country | Brand | Strength | Notes |
|---|---|---|---|---|
| Natco Pharma Ltd. | India | Bracanat | 100 mg and 150 mg tablets | Received USFDA tentative approval for generic olaparib tablets |
| Beacon Pharmaceuticals PLC | Bangladesh | Olapar | 100 mg and 150 mg tablets | Listed on MedEx with Bangladesh the data |
| Incepta Pharmaceuticals Ltd. | Bangladesh | Olacent | 100 mg and 150 mg tablets | Listed on MedEx; notably lower the datad than other Bangladeshi brands |
| Everest Pharmaceuticals Ltd. | Bangladesh | Olanib | 150 mg tablet and 50 mg capsule | Listed on MedEx and on Everest's own store |
Availability in Southeast Asia
| Country | Status | Notes |
|---|---|---|
| Singapore | approved | Approved by the Health Sciences Authority (HSA); olaparib is also listed in the Singapore National Drug Formulary |
| Malaysia | approved | Approved by the National Pharmaceutical Regulatory Agency (NPRA) for certain ovarian and breast cancers |
| Thailand | approved | Approved by the Thai FDA for advanced ovarian and breast cancers with BRCA mutations |
| Philippines | approved | Approved by the Philippines FDA for BRCA-mutated ovarian and breast cancers; use in specialised oncology centres |
| Vietnam | approved | Approved by the Drug Administration of Vietnam (DAV) for certain cancers including BRCA-mutated ovarian and breast cancer |
| Brunei | not approved | No publicly accessible data on approval status by Brunei's Ministry of Health |
| Cambodia | not approved | Approval status not documented in publicly accessible regulatory databases |
Frequently asked questions
Is there a generic olaparib available and who makes it?
Natco Pharma's generic olaparib tablets (100 mg and 150 mg) received USFDA tentative approval, meaning the formulation met the regulatory requirements for bioequivalence, safety, efficacy and quality against the reference listed drug Lynparza. Bangladeshi olaparib products (Beacon Olapar, Incepta Olacent, Everest Olanib) are DGDA-registered and made under the TRIPS least-developed-country patent exemption, not as FDA/EMA-approved generics; no published BE study against Lynparza was found for them. Manufacturers supplying olaparib generic versions include Beacon Pharmaceuticals PLC, Everest Pharmaceuticals Ltd. , Incepta Pharmaceuticals Ltd. , Natco Pharma Ltd. . Brands registered in Bangladesh include Inpoza, Juparib, Lynparib, Olacent, Olakin, Olanib.
What is the difference between olaparib and niraparib?
Olaparib (PARP inhibitor (poly (ADP-ribose) polymerase inhibitor), originally Lynparza by AstraZeneca (distributed by AstraZeneca Pharmaceuticals LP); developed and commercialised in collaboration with Merck (MSD outside the US and Canada)) Olaparib blocks PARP, an enzyme that cancer cells use to repair damaged DNA. Cancer cells that already have a faulty DNA-repair gene (such as BRCA1 or BRCA2) cannot fix the damage when PARP is also blocked, so they die. It is used mostly in cancers linked to BRCA mutations - ovarian, breast, pancreatic and prostate cancer. 300 mg (two 150 mg tablets) taken orally twice daily, with or without food (total daily dose 600 mg). Continue until disease progression or unacceptable toxicity; for first-line maintenance of BRCA-mutated advanced ovarian cancer, continue until progression, unacceptable toxicity, or completion of 2 years of treatment.
Do I need a BRCA test before taking olaparib?
Recommended monitoring for olaparib: Complete blood count for cytopenia at baseline and monthly thereafter for clinically significant changes during treatment (monitor for MDS/AML); For prolonged haematological toxicity, interrupt treatment and monitor blood counts weekly until recovery; if not recovered to Grade 1 or less after 4 weeks, refer to a haematologist including bone marrow analysis; Monitoring for new or worsening respiratory symptoms (dyspnea, cough, fever) or radiological abnormality that could indicate pneumonitis; Do not start until patients have recovered from haematological toxicity caused by previous chemotherapy (<=Grade 1)
How long do you take olaparib as maintenance for ovarian cancer?
Olaparib (PARP inhibitor (poly (ADP-ribose) polymerase inhibitor), originally Lynparza by AstraZeneca (distributed by AstraZeneca Pharmaceuticals LP); developed and commercialised in collaboration with Merck (MSD outside the US and Canada)) Olaparib blocks PARP, an enzyme that cancer cells use to repair damaged DNA. Cancer cells that already have a faulty DNA-repair gene (such as BRCA1 or BRCA2) cannot fix the damage when PARP is also blocked, so they die. It is used mostly in cancers linked to BRCA mutations - ovarian, breast, pancreatic and prostate cancer. 300 mg (two 150 mg tablets) taken orally twice daily, with or without food (total daily dose 600 mg). Continue until disease progression or unacceptable toxicity; for first-line maintenance of BRCA-mutated advanced ovarian cancer, continue until progression, unacceptable toxicity, or completion of 2 years of treatment.
Is olaparib available in Singapore, Malaysia or the Philippines?
Olaparib is made by 4 suppliers tracked in this database, including Beacon Pharmaceuticals PLC, Everest Pharmaceuticals Ltd. , Incepta Pharmaceuticals Ltd. , Natco Pharma Ltd. . Bangladesh-registered brands: Inpoza, Juparib, Lynparib, Olacent, Olakin, Olanib, Olapar, Olarigen, Olatab, Ovarib.
Does olaparib cause hair loss?
Olaparib (PARP inhibitor (poly (ADP-ribose) polymerase inhibitor), originally Lynparza by AstraZeneca (distributed by AstraZeneca Pharmaceuticals LP); developed and commercialised in collaboration with Merck (MSD outside the US and Canada)) Olaparib blocks PARP, an enzyme that cancer cells use to repair damaged DNA. Cancer cells that already have a faulty DNA-repair gene (such as BRCA1 or BRCA2) cannot fix the damage when PARP is also blocked, so they die. It is used mostly in cancers linked to BRCA mutations - ovarian, breast, pancreatic and prostate cancer. 300 mg (two 150 mg tablets) taken orally twice daily, with or without food (total daily dose 600 mg). Continue until disease progression or unacceptable toxicity; for first-line maintenance of BRCA-mutated advanced ovarian cancer, continue until progression, unacceptable toxicity, or completion of 2 years of treatment.
What is the risk of MDS or AML with olaparib?
Olaparib (PARP inhibitor (poly (ADP-ribose) polymerase inhibitor), originally Lynparza by AstraZeneca (distributed by AstraZeneca Pharmaceuticals LP); developed and commercialised in collaboration with Merck (MSD outside the US and Canada)) Olaparib blocks PARP, an enzyme that cancer cells use to repair damaged DNA. Cancer cells that already have a faulty DNA-repair gene (such as BRCA1 or BRCA2) cannot fix the damage when PARP is also blocked, so they die. It is used mostly in cancers linked to BRCA mutations - ovarian, breast, pancreatic and prostate cancer. 300 mg (two 150 mg tablets) taken orally twice daily, with or without food (total daily dose 600 mg). Continue until disease progression or unacceptable toxicity; for first-line maintenance of BRCA-mutated advanced ovarian cancer, continue until progression, unacceptable toxicity, or completion of 2 years of treatment.
Can olaparib be used for pancreatic or prostate cancer?
Olaparib is approved for: Maintenance treatment of adults with deleterious or suspected deleterious germline or somatic BRCA-mutated advanced epithelial ovarian, fallopian tube or primary peritoneal cancer in complete or partial response to first-line platinum-based chemotherapy; In combination with bevacizumab, maintenance treatment of adults with advanced epithelial ovarian, fallopian tube or primary peritoneal cancer in complete or partial response to first-line platinum-based chemotherapy whose cancer is HRD-positive (BRCA mutation and/or genomic instability); Maintenance treatment of adults with recurrent epithelial ovarian, fallopian tube or primary peritoneal cancer in complete or partial response to platinum-based chemotherapy; Treatment of adults with deleterious or suspected deleterious germline BRCA-mutated advanced ovarian cancer who have been treated with three or more prior lines of chemotherapy; Treatment of adults with deleterious or suspected deleterious gBRCAm, HER2-negative metastatic breast cancer who have been treated with chemotherapy in the neoadjuvant, adjuvant or metastatic setting. It is a olaparib (PARP inhibitor), originally marketed as Lynparza by AstraZeneca (distributed by AstraZeneca Pharmaceuticals LP); developed and commercialised in collaboration with Merck (MSD outside the US and Canada).
Why must I avoid grapefruit while taking olaparib?
Olaparib (PARP inhibitor (poly (ADP-ribose) polymerase inhibitor), originally Lynparza by AstraZeneca (distributed by AstraZeneca Pharmaceuticals LP); developed and commercialised in collaboration with Merck (MSD outside the US and Canada)) Olaparib blocks PARP, an enzyme that cancer cells use to repair damaged DNA. Cancer cells that already have a faulty DNA-repair gene (such as BRCA1 or BRCA2) cannot fix the damage when PARP is also blocked, so they die. It is used mostly in cancers linked to BRCA mutations - ovarian, breast, pancreatic and prostate cancer. 300 mg (two 150 mg tablets) taken orally twice daily, with or without food (total daily dose 600 mg). Continue until disease progression or unacceptable toxicity; for first-line maintenance of BRCA-mutated advanced ovarian cancer, continue until progression, unacceptable toxicity, or completion of 2 years of treatment.
Sources
- https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/208558s013lbl.pdf
- https://www.fda.gov/drugs/fda-approved-olaparib-lynparza-astrazeneca-pharmaceuticals-lp-maintenance-treatment-adult-patients
- https://www.astrazeneca.com/media-centre/press-releases/2020/lynparza-approved-in-the-us-for-hrr-gene-mutated-metastatic-castration-resistant-prostate-cancer.html
- https://medex.com.bd/generics/1399/olaparib
- https://medex.com.bd/generics/1399/olaparib/brand-names
- https://www.oncnursingnews.com/view/fda-grants-tentative-approval-to-generic-olaparib-tablets
- https://everyone.org/lynparza-olaparib
- https://www.1mg.com/drugs/lynparza-150mg-tablet-688784
- https://www.netmeds.com/product/lynparza-100mg-tablet-8s-lufum0-7520077
This page is an information resource for healthcare professionals, licensed importers and patients under medical care. It is not medical advice, not a prescription service, and not an offer to sell prescription medicines to the public.
Related molecules in the same therapeutic area
Need a verified quotation?
Send us the molecule, strength, pack size, quantity and destination country. We reply with a batch-traceable quotation, certificates of analysis and shipping documentation.
We supply licensed pharmacies, hospitals, importers and distributors — not direct-to-consumer patients.
