The Medical Letter on Drugs and Therapeutics
Olaparib (Lynparza) for Advanced Ovarian Cancer (online only)
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The FDA has approved the oral poly (ADP-ribose) polymerase (PARP) inhibitor olaparib (Lynparza – Astra-Zeneca) as monotherapy for treatment of women with advanced ovarian cancer who have BRCA1/2 germline mutations and have received at least 3 prior lines of chemotherapy. Olaparib is the first PARP inhibitor to be approved in the US. It is approved outside the US for maintenance treatment of relapsed BRCA-mutated ovarian cancer.

MECHANISM OF ACTION — PARP enzymes are involved in many cellular functions, including DNA transcription and repair. PARP inhibition causes breaks in double-stranded DNA. Olaparib is most active against tumors with a deficiency in homologous recombination (DNA repair), such as those with BRCA1/2 mutations, because it activates an ineffective repair mechanism, a process known as synthetic lethality. It is cytotoxic for ovarian cancer cells in general, but especially for those that ... more      

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Title: Olaparib (Lynparza) for Advanced Ovarian Cancer (online only)
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