Olaparib

BeschreibungOlaparib, marketed by AstraZeneca under the brand name Lynparza , was approved in the USA in December 2014 as a targeted, single-agent therapy for the treatment of germline BRCA-mediated advanced ovarian cancer.Olaparib, originally developed by KuDOS pharmaceuticals and later by AstraZeneca, functions as a poly ADP ribose polymerase inhibitor and has been specifically approved for patients who have received three or more treatments of chemotherapy. In clinical trials, the drug prolonged progression- free survival for patients suffering from platinum-sensitive recurrent serous ovarian cancer. Olaparib is also currently in various phases of investigation for treatment of breast, gastric, prostate, pancreatic and non-small cell lung cancer.

HistoryOlaparib, the first approved small molecule PARPi, is utilized for the treatment of germline BRCA-mutated ovarian and breast cancers. Olaparib was discovered by Professor Sir Steve Jackson, it was developed and first dosed into patients by the UK-based biotechnology company, KuDOS Pharmaceuticals, that was founded by Stephen Jackson of Cambridge University, UK. Since KuDOS was acquired by AstraZeneca in 2006, the drug has undergone clinical development by AstraZeneca and Merck & Co.

VerwendenOlaparib is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Olaparib has been shown to induce significant killing of ATM-deficient lymphoid tumor cells in vitro and in vivo. Recent studies show that Olaparib increases radiosensitivity of a lung tumor xenograft, making it a potential candidate for use in combination with radiotherapy.

DefinitionChEBI: Olaparib is a member of the class of N-acylpiperazines obtained by formal condensation of the carboxy group of 2-fluoro-5-[(4-oxo-3,4-dihydrophthalazin-1-yl)methyl]benzoic acid with the free amino group of N-(cyclpropylcarbonyl)piperazine; used to treat advanced ovarian cancer. It has a role as an antineoplastic agent, an EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor and an apoptosis inducer. It is a N-acylpiperazine, a member of cyclopropanes, a member of monofluorobenzenes and a member of phthalazines.