Olaparib - CAS 763113-22-0
Catalog number: 763113-22-0
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Olaparib, also known as AZD-2281 or KU-59436, is a small molecule inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with 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. PARP catalyzes post-translational ADP-ribosylation of nuclear proteins and can be activated by single-stranded DNA breaks.
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white solid powder
KU-59436, KU-0059436. AZD2281; AZD=2281; AZD 2281;
1.Synthesis of Olaparib Derivatives and Their Antitumor Activities
LOU Xi-yu, YANG Xuan. Chem. Res. Chin. Univ. 2013, 29(2), 231—235
In order to improve its antitumor effects and discover more potent and effective antitumor agents, our group performed chemical modification of Olaparib(modification sites are shown in Fig.1), synthesized a series of Olaparib analogues and evaluated their in vitro antitumor activities against BRCA1-deficient cell lines HCC1937, Capan-1 and MDA-MB-436. We herein report the synthesis of these compounds, and their in vitro antitumor activity. The synthetic routes of the target compounds are outlined in Schemes 1 and 2.
2.A Phase I study of olaparib and irinotecan in patients with colorectal cancer: Canadian Cancer Trials Group IND 187
Eric X. Chen & Derek J. Jonker & Lillian L. Siu. Invest New Drugs (2016) 34:450–457
In preclinical studies, olaparib and other PARP inhibitors were shown to potentiate the anti-tumor effect of topoisomer ase I inhibitors, such as irinotecan, and combining PARP and topoisomerase I inhibitors was considered to be a potential therapeutic strategy. We conducted a phase I study to evaluate the safety and tolerability of olaparib in combination with irinotecan, and to determine the recommended phase II dose (RP2D) of this combination in patients with advanced colorectal cancer (NCT00535353). Secondary objectives included determining olaparib pharmacokinetics with and without irinotecan, irinotecan pharmacokinetics in the presence of olaparib, and collecting preliminary evidence of anti-tumor activity.
3.Evaluation of the pharmacodynamics and pharmacokinetics of the PARP inhibitor olaparib: a Phase I multicentre trial in patients scheduled for elective breast cancer surgery
Nigel Bundred & Janis Gardovskis & Janusz Jaskiewicz. Invest New Drugs (2013) 31:949–958
Tumour exposure to olaparib was achieved in all but one of the post-treatment samples obtained from patients dosed with olaparib 30 mg bid and above; the exception was the tumour sample from one patient in the 200 mg bid dose group. Within the 10 mg bid group, olaparib could not be detected in the post-treatment tumour tissue samples from seven patients, and was less than 100 ng/g in samples from a further two patients (assay LOQ=40 ng/g). As with the plasma measurements, wide inter-patient variability was observed in the olaparib concentrations in tumour tissue samples (Fig. 1c); no clear dose-exposure relationship was evident in these samples.
4.Olaparib: a promising PARP inhibitor in ovarian cancer therapy
Ying Chen • Lei Zhang • Quan Hao. Arch Gynecol Obstet (2013) 288:367–374
However, a comprehensive understanding of the therapeutic applications of Olaparib in tumor cells was not available until recently. Within this review, we briefly summarize the recent research progress on the efficacy and tolerability of Olaparib in OC patients with or without BRCA mutation. Hopefully the information in this article summarizing the recent studies advances will lead to a better understand of the mechanisms of Olaparib in genome stability maintenance and provide valuable clues in the selection of patient populations that will respond to Olaparib.
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