Lynparza (olaparib; AstraZeneca/Merck & Co) is a small molecule poly (ADP-ribose) polymerase (PARP) inhibitor for the treatment of BRCA mutation-positive (BRCAm+) ovarian cancer.
The PARP enzyme plays an essential role in DNA repair mechanisms and homologous recombination events. PARP inhibitors act by directly blocking enzymatic activity, or by causing PARP to accumulate on DNA (PARP trapping), which results in DNA replication inhibition and cell death. Tumor cells with BRCA1/2 gene mutations are dependent on PARP for DNA damage repair, and PARP inhibition selectively kills BRCA1- or BRCA2-deficient cells. As DNA repair is inhibited by PARP inhibitors, they are often sequenced after a cytotoxic chemotherapy which works by damaging DNA.
BRCA1 and BRCA2 encode proteins that are required for DNA damage repair. Inherited mutations in these genes have been linked to a predisposition towards the development of breast and ovarian cancers. In the US, it has been estimated that inherited BRCA1 and BRCA2 mutations account for 5-10% of breast cancers and 10-15% of ovarian cancers among white women.
The drug is also being developed by AstraZeneca and Merck & Co for the treatment of prostate cancer.
- Lynparza: Prostate cancer
- Lynparza: Ovarian cancer
- Lynparza: Breast cancer: triple-negative
- Lynparza: Pancreatic cancer
- Lynparza: Breast cancer: HR+/HER2-
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