Overview
Olaparib is a selective and potent inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, PARP1 and PARP2. PARP inhibitors represent a novel class of anti-cancer therapy and they work by taking advantage of a defect in DNA repair in cancer cells with BRCA mutations and inducing cell death. Olaparib is used to treat a number of BRCA-associated tumours, including ovarian cancer, breast cancer, pancreatic cancer, and prostate cancer. It was first approved by the FDA and EU in December 2014, and by Health Canada in April 2016.
Indication
Ovarian cancer Olaparib is indicated for the maintenance treatment of adults 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. Olaparib is indicated in combination with bevacizumab for the maintenance treatment of adults 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. Olaparib is indicated for the maintenance treatment of adult patients with recurrent epithelial ovarian, fallopian tube or primary peritoneal cancer, who are in complete or partial response to platinum-based chemotherapy. Breast cancer Olaparib is indicated for the adjuvant treatment of adult patients with deleterious or suspected deleterious gBRCAm human epidermal growth factor receptor 2 (HER2)-negative high risk early breast cancer who have been treated with neoadjuvant or adjuvant chemotherapy. Olaparib is indicated for the treatment of adult patients with deleterious or suspected deleterious gBRCAm, HER2-negative metastatic breast cancer, who have been treated with chemotherapy in the neoadjuvant, adjuvant, or metastatic setting. Patients with hormone receptor (HR) positive breast cancer should have been treated with a prior endocrine therapy or be considered inappropriate for endocrine therapy. Pancreatic cancer Olaparib is indicated for the maintenance treatment of adult patients with deleterious or suspected deleterious gBRCAm metastatic pancreatic adenocarcinoma whose disease has not progressed on at least 16 weeks of a first-line platinum-based chemotherapy regimen. Prostate cancer Olaparib is indicated for the treatment of adult patients 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 a hormone agent, such as enzalutamide or abiraterone. It is also indicated in combination with abiraterone and prednisone or prednisolone for the treatment of adult patients with deleterious or suspected deleterious BRCA-mutated (BRCAm) metastatic castration-resistant prostate cancer (mCRPC).
Associated Conditions
- Advanced Epithelial Ovarian Cancer
- Advanced Fallopian Tube Carcinoma
- Advanced Primary Peritoneal Carcinoma
- High risk, early breast cancer
- Hormone Receptor Positive Breast Carcinoma
- Locally Advanced Breast Cancer (LABC)
- Metastatic Adenocarcinoma of the Pancreas
- Metastatic Breast Cancer
- Metastatic Castration-Resistant Prostate Cancer (mCRPC)
- Pancreatic Adenocarcinoma Metastatic
- Recurrent Epithelial Ovarian Cancer
- Recurrent Fallopian Tube Cancer
- Stage I Breast Cancer
- Advanced high-grade epithelial ovarian cancer
- Advanced, high-grade Primary Peritoneal Cancer
- High-grade advanced Fallopian Tubes Cancer
- Recurrent platinum sensitive primary peritoneal cancer
- Relapsed Platinum-Sensitive Epithelial Ovarian Cancer
- Relapsed platinum sensitive primary peritoneal cancer
- Relapsed platinum-sensitive fallopian tube cancer
Research Report
Olaparib (Lynparza®): A Comprehensive Clinical and Pharmacological Monograph
I. Executive Summary
Olaparib, marketed as Lynparza®, is a first-in-class, orally administered small molecule inhibitor of poly(ADP-ribose) polymerase (PARP) enzymes. It represents a paradigm of targeted therapy, leveraging the principle of synthetic lethality to selectively induce cytotoxicity in tumors with deficiencies in the homologous recombination repair (HRR) pathway, most notably those with deleterious BRCA1 or BRCA2 mutations. This mechanism provides a wide therapeutic index, effectively targeting cancer cells while relatively sparing normal cells.
The drug has secured landmark approvals from the U.S. Food and Drug Administration (FDA) and the European Medicines Agency (EMA) for the treatment of specific, biomarker-defined patient populations across four major cancer types: ovarian, breast, prostate, and pancreatic cancer.[1] Its indications have evolved significantly, moving from late-line salvage therapy for heavily pre-treated patients to first-line maintenance and adjuvant settings, fundamentally altering the standards of care for eligible individuals.[2]
The clinical efficacy of Olaparib is supported by a robust portfolio of pivotal Phase III trials. Studies such as SOLO-1, SOLO-2, and PAOLA-1 in ovarian cancer; OlympiA in early breast cancer; PROfound in prostate cancer; and POLO in pancreatic cancer have consistently demonstrated statistically significant and clinically meaningful improvements in progression-free survival (PFS).[4] In certain settings, particularly the adjuvant treatment of early breast cancer, this has translated into a significant overall survival (OS) benefit, establishing Olaparib as a cornerstone of care for patients with susceptible tumors.[7]
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2025/06/17 | Phase 2 | Not yet recruiting | |||
2025/05/13 | Phase 3 | Recruiting | |||
2025/04/07 | Phase 3 | Recruiting | |||
2025/04/04 | Phase 2 | Recruiting | |||
2025/03/04 | Phase 1 | Not yet recruiting | |||
2025/01/28 | Phase 2 | Recruiting | |||
2025/01/20 | N/A | Recruiting | Santa Chiara Hospital | ||
2024/12/18 | Phase 2 | Recruiting | Tianjin Medical University Second Hospital | ||
2024/12/02 | Phase 3 | Recruiting | |||
2024/11/13 | Phase 2 | Recruiting |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| AstraZeneca Pharmaceuticals LP | 0310-0679 | ORAL | 150 mg in 1 1 | 11/6/2023 | |
| AstraZeneca Pharmaceuticals LP | 0310-0668 | ORAL | 100 mg in 1 1 | 11/6/2023 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
Authorised | 12/16/2014 |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| LYNPARZA FILM-COATED TABLET 100MG | SIN15663P | TABLET, FILM COATED | 100mg | 4/9/2019 | |
| LYNPARZA FILM-COATED TABLET 150MG | SIN15662P | TABLET, FILM COATED | 150mg | 4/9/2019 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| Olaparib Tablets | m/s natco pharma limited | 国药准字HJ20250005 | 化学药品 | 片剂 | 1/8/2025 |
| Olaparib Tablets | m/s natco pharma limited | 国药准字HJ20250006 | 化学药品 | 片剂 | 1/8/2025 |
| Olaparib Tablets | 国药准字H20244040 | 化学药品 | 片剂 | 6/18/2024 | |
| Olaparib Tablets | 国药准字H20233531 | 化学药品 | 片剂 | 5/12/2023 | |
| Olaparib Tablets | 国药准字H20243888 | 化学药品 | 片剂 | 6/4/2024 | |
| Olaparib Tablets | 国药准字H20243822 | 化学药品 | 片剂 | 5/28/2024 | |
| Olaparib Tablets | 国药准字H20243063 | 化学药品 | 片剂 | 1/16/2024 | |
| Olaparib Tablets | 国药准字H20243813 | 化学药品 | 片剂 | 5/28/2024 | |
| Olaparib Tablets | 国药准字H20233532 | 化学药品 | 片剂 | 5/12/2023 | |
| Olaparib Tablets | 国药准字HJ20180049 | 化学药品 | 片剂 | 3/20/2023 |
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| No PPB approvals found for this drug. | |||||
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| LYNPARZA olaparib 150 mg film coated tablet blister pack | 288614 | Medicine | A | 5/23/2018 | |
| LYNPARZA olaparib 100 mg film coated tablet blister pack | 288613 | Medicine | A | 5/23/2018 |
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