Olaparib (AZD2281; KU0059436)

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.

AZD2281, Ku-0059436; AZD2281; AZD-2281; AZD 2281; KU59436; KU-59436; KU 59436; KU0059436; KU-0059436; KU 0059436; Olaparib. trade name Lynparza

Chemical Name: 4-[[3-[4-(cyclopropanecarbonyl)piperazine-1-carbonyl]-4-fluorophenyl]methyl]-2H-phthalazin-1-one

SMILES Code: O=C1NN=C(CC2=CC=C(F)C(C(N3CCN(C(C4CC4)=O)CC3)=O)=C2)C5=C1C=CC=C5