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Drugs. 2017 Jun;77(9):1029-1034. doi: 10.1007/s40265-017-0752-y.
Oral niraparib, a highly-selective, potent poly(ADP-ribose) polymerase (PARP)-1 and PARP-2 inhibitor, is approved in the USA for the maintenance treatment of adult patients with recurrent epithelial ovarian, fallopian tube or primary peritoneal cancer who are in a complete or partial response to platinum-based chemotherapy. It is also under regulatory review in the EU for use in maintenance treatment in patients with platinum-sensitive, recurrent epithelial ovarian cancer who are in response to platinum-based chemotherapy. In the multinational, phase 3 NOVA trial in adult patients with platinum-sensitive, recurrent ovarian cancer, niraparib significantly prolonged median progression-free survival, irrespective of the presence or absence of a germline BRCA (gBRCA) mutation and irrespective of the presence or absence of homologous recombinant deficiency. Niraparib is also in development for use in other solid tumours, including breast and prostate cancer. This article summarizes the milestones in the development of niraparib leading to its first global approval for the maintenance treatment of adult patients with recurrent epithelial ovarian, fallopian tube or primary peritoneal cancer.
尼拉帕利口服制剂是一种高选择性、强效的多聚（ADP-核糖）聚合酶（PARP）-1 和 PARP-2 抑制剂，已获美国批准用于铂类化疗完全或部分缓解后的复发性上皮性卵巢癌、输卵管癌或原发性腹膜癌成人患者的维持治疗。该药也正在接受欧盟监管审查，拟用于对铂类化疗有反应的铂类敏感、复发性上皮性卵巢癌患者的维持治疗。在一项针对铂类敏感、复发性卵巢癌成人患者的多中心、3 期 NOVA 试验中，尼拉帕利显著延长了中位无进展生存期，无论是否存在种系 BRCA（gBRCA）突变以及同源重组缺陷是否存在。尼拉帕利也正在开发用于治疗其他实体瘤，包括乳腺癌和前列腺癌。本文总结了尼拉帕利开发过程中的重要里程碑，最终该药在全球首次获批，用于铂类化疗完全或部分缓解后的复发性上皮性卵巢癌、输卵管癌或原发性腹膜癌成人患者的维持治疗。
