Description: Olaparib (formerly also known as AZD-2281; KU-59436; KU0059436; trade name Lynparza) is a potent, novel and orally bioavailable small molecule inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential anticancer activity. It inhibits PARP with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. It has potential chemosensitizing, radiosensitizing, and antineoplastic activities. Olaparib selectively binds to and inhibits PARP, inhibiting PARP-mediated repair of single strand DNA breaks; PARP inhibition may enhance the cytotoxicity of DNA-damaging agents and may reverse tumor cell chemoresistance and radioresistance. Olaparib was approved in 2014 by FDA for treating advanced ovarian cancer.
References: J Med Chem. 2008 Oct 23;51(20):6581-91; Proc Natl Acad Sci U S A. 2008 Nov 4;105(44):17079-84.
Publications Citing Use of InvivoChem Olaparib (AZD2281; KU0059436): medRxiv preprint doi: https://doi.org/10.1101/2022.12.02.22283037