Olaparib: an oral PARP-1 and PARP-2 inhibitor with promising activity in ovarian cancer
Olaparib: an oral PARP-1 and PARP-2 inhibitor with promising activity in ovarian cancer
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DOI：
10.2217/fon.14.313
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发表时间：
2015-01-01
期刊：
影响因子：
3.3
通讯作者：
Moore, Kathleen N.
中科院分区：
文献类型：
--
作者：
Gunderson, Camille C.;Moore, Kathleen N.
奥拉帕尼（Lynparza（TM）; AZD 2281）是一种有效的PARP-1和PARP-2抑制剂，在卵巢癌以及其他实体瘤中具有生物活性。它已在I期和II期试验中进行了测试，并在生殖系BRCA突变和散发性卵巢癌中具有单药活性。考虑到与药物作用机制的内在分子相容性，正在进行III期试验，评估奥拉帕尼在一线和铂敏感性复发后维持治疗中对生殖系BRCA突变患者的疗效。
Olaparib (Lynparza (TM); 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.