In December 2014, olaparib was approved for use as a single agent by the In August 2017, olaparib tablets were approved in the United States for the maintenance treatment of adults with recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer, who are in a complete or partial response to platinum-based chemotherapy.The approval in the maintenance setting was based on two randomized, placebo-controlled, double-blind, multicenter trials in patients with recurrent ovarian cancers who were in response to platinum-based therapy.In January 2018, olaparib was approved in the United States for the treatment of patients with certain types of breast cancer that have spread (metastasized) and whose tumors have a specific inherited (germline) genetic mutation, making it the first drug in its class (PARP inhibitor) approved to treat breast cancer, and it is the first time any drug has been approved to treat certain patients with metastatic breast cancer who have a “BRCA” gene mutation.In December 2018, olaparib was approved in the United States for the maintenance treatment of adults with deleterious or suspected deleterious germline or somatic BRCA-mutated (gBRCAm or sBRCAm) advanced epithelial ovarian, fallopian tube or primary peritoneal cancer who are in complete or partial response to first-line platinum-based chemotherapy.In December 2019, olaparib was approved for the maintenance treatment of adults with deleterious or suspected deleterious germline BRCA-mutated (gBRCAm) metastatic pancreatic adenocarcinoma, as detected by an FDA-approved test, whose disease has not progressed on at least 16 weeks of a first-line platinum-based chemotherapy regimen.An April 2020 clinical trial indicated that olaparib treatment resulted in longer survival for patients with metastatic castration-resistant prostate cancer compared to c4cccc2c4c(n[nH]c2=O)Cc(ccc1F)cc1C(=O)N3CCN(CC3)C(=O)C5CC5InChI=1S/C24H23FN4O3/c25-20-8-5-15(14-21-17-3-1-2-4-18(17)22(30)27-26-21)13-19(20)24(32)29-11-9-28(10-12-29)23(31)16-6-7-16/h1-5,8,13,16H,6-7,9-12,14H2,(H,27,30)4-[(3-[(4-cyclopropylcarbonyl)piperazin-1-yl]carbonyl) -4-fluorophenyl]methyl(2H)phthalazin-1-one Learn about the LYNPARZA® (olaparib) mechanism of action as a PARP inhibitor in first-line maintenance for women with sBRCA- or gBRCA-mutated advanced ovarian cancer.

Learn about the LYNPARZA® (olaparib) mechanism of action as a PARP inhibitor for patients with gBRCAm HER2-negative metastatic breast cancer who have been treated with chemotherapy in any setting and if HR+, endocrine therapy.

Lactation: No data are available regarding the presence of olaparib in human milk, its effects on the breastfed infant or on milk production. Olaparib inhibits the PARP‐mediated error‐free repair of SSB, resulting in synthetic lethality in BRCA‐associated cancer cells as DNA is then repaired with more error‐prone repair mechanisms – single‐strand annealing and non‐homologous end joining 3.

Discontinue LYNPARZA if Most common adverse reactions (Grades 1-4) in ≥10% of patients in clinical trials of LYNPARZA in the Most common laboratory abnormalities (Grades 1-4) in ≥25% of patients in clinical trials of LYNPARZA in the In addition, venous thromboembolic events occurred more commonly in patients receiving LYNPARZA/bevacizumab (5%) than in those receiving placebo/bevacizumab (1.9%).Most common laboratory abnormalities (Grades 1-4) in ≥25% of patients for LYNPARZA in combination with bevacizumab in the Most common adverse reactions (Grades 1-4) in ≥20% of patients in clinical trials of LYNPARZA in the Most common laboratory abnormalities (Grades 1-4) in ≥25% of patients in clinical trials of LYNPARZA in the Most common adverse reactions (Grades 1-4) in ≥20% of patients in clinical trials of LYNPARZA for Most common laboratory abnormalities (Grades 1-4) in ≥25% of patients in clinical trials of LYNPARZA for Most common adverse reactions (Grades 1-4) in ≥20% of patients in Most common laboratory abnormalities (Grades 1-4) in ≥25% of patients in Most common adverse reactions (Grades 1-4) in ≥10% of patients in clinical trials of LYNPARZA in the Most common laboratory abnormalities (Grades 1-4) in ≥25% of patients in clinical trials of LYNPARZA in the You may report side effects related to AstraZeneca products by clicking LYNPARZA is a registered trademark and AZ&Me and AstraZeneca Access 360 are trademarks of the AstraZeneca group
For prolonged hematological toxicities, interrupt LYNPARZA and monitor blood count weekly until recovery.If the levels have not recovered to Grade 1 or less after 4 weeks, refer the patient to a hematologist for further investigations, including bone marrow analysis and blood sample for cytogenetics.

Tumor cells survive by repairing their damaged DNA via the PARP enzyme, among other Disrupting the DNA-repair process with a PARPi may help drive LYNPARZA targets PARP to disrupt the DNA-repair process and potentially kill tumor cellsTumor cells survive by repairing their damaged DNA via the PARP enzyme, among other Disrupting the DNA-repair process with a PARP inhibitor may help drive In vitro studies have shown that olaparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of trapped PARP-DNA complexes, resulting in DNA damage and cancer-cell death. Myelodysplastic Syndrome/Acute Myeloid Leukemia (MDS/AML):

BRCA1/2mutations may be genetically predisposed to development of some forms of cancer, and may be resistant to other forms of cancer treatment.
Mechanism of action. Jane Robertson, MD, Global Product Vice President of Oncology at AstraZeneca, describes the mechanism of action of olaparib, a PARP inhibitor. Olaparib acts as an inhibitor of the enzyme poly ADP ribose polymerase (PARP), and is termed a PARP inhibitor. Because of the potential for serious adverse reactions in the breastfed infant, advise a lactating woman not to breastfeed during treatment with LYNPARZA and for 1 month after receiving the final dose. Olaparib is extensively metabolized in the liver by the action of CYP3A isoenzymes. [F2974] From the administered dose, the unchanged form of olaparib accounted for 70% of the circulating dose and it was considered the major component in urine and feces. If PARP is inhibited, single strand breaks cannot be repaired efficiently.


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