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奥拉帕利:一种口服聚(ADP-核糖)聚合酶-1和聚(ADP-核糖)聚合酶-2抑制剂,在卵巢癌中具有显著活性。

Olaparib: an oral PARP-1 and PARP-2 inhibitor with promising activity in ovarian cancer.

作者信息

Gunderson Camille C, Moore Kathleen N

机构信息

University of Oklahoma Health Sciences Center, Stephenson Oklahoma Cancer Center, 800 NE 10th Street, Suite 5040, Oklahoma City, OK 73104, USA.

出版信息

Future Oncol. 2015;11(5):747-57. doi: 10.2217/fon.14.313.

Abstract

Olaparib (Lynparza™; AZD2281) is a potent PARP-1 and PARP-2 inhibitor with biologic activity in ovarian cancer as well as other solid tumors. It has been tested in Phase I and II trials and has single-agent activity in both germline BRCA mutated and sporadic ovarian cancer. Phase III trials assessing the efficacy of olaparib in the maintenance setting following first line and platinum-sensitive recurrence are underway for patients with a germline BRCA mutation, given the inherent molecular compatibility with the drug's mechanism of action.

摘要

奥拉帕利(Lynparza™;AZD2281)是一种强效的聚(ADP-核糖)聚合酶-1(PARP-1)和聚(ADP-核糖)聚合酶-2(PARP-2)抑制剂,对卵巢癌以及其他实体瘤具有生物活性。它已在I期和II期试验中进行了测试,对胚系BRCA突变型和散发性卵巢癌均具有单药活性。鉴于与该药物作用机制具有内在分子相容性,针对胚系BRCA突变患者的III期试验正在评估奥拉帕利在一线治疗和铂敏感复发后的维持治疗中的疗效。

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