a Division of Gynecologic Oncology , University of Oklahoma Stephenson Cancer Center , Oklahoma City , USA.
Expert Rev Anticancer Ther. 2018 Aug;18(8):727-733. doi: 10.1080/14737140.2018.1490180. Epub 2018 Jul 2.
Niraparib, an orally available selective inhibitor of poly(adenosine diphosphate-ribose) polymerase (PARP), is the first PARP inhibitor approved for use in patients with ovarian cancer who do not harbor a germ-line or somatic mutation in the breast cancer gene (BRCA). Overall, niraparib is well tolerated and its toxicities, primarily hematologic, are manageable especially with recently released initial dose modification guidelines based on weight and baseline platelet count. The role of niraparib as maintenance following frontline platinum-based chemotherapy as well as in the treatment of recurrent high-grade serous ovarian cancer is an active area of investigation. Areas covered: This review focuses on niraparib, its pharmacology, clinical efficacy, and adverse effects as evidenced by prospective clinical trials, and licensed indications. Expert commentary: Niraparib introduced the use of PARP inhibitors regardless of biomarker status. Recent studies highlight the critical need for more accurate biomarkers to identify patients most likely to benefit from treatment with PARP inhibitors. In the next 5 years, we anticipate further expansion of and elucidation regarding the optimal indication for use of niraparib in the treatment of ovarian cancer.
尼拉帕利是一种口服聚（二磷酸腺苷核糖）聚合酶（PARP）选择性抑制剂，是首个获批用于治疗卵巢癌的 PARP 抑制剂，适用患者为不携带乳腺癌基因（BRCA）种系或体细胞突变的患者。总体而言，尼拉帕利具有良好的耐受性，其毒性主要是血液学毒性，尤其在最近根据体重和基线血小板计数发布的初始剂量调整指南后，毒性可管理。尼拉帕利在一线铂类化疗后的维持治疗以及复发性高级别浆液性卵巢癌的治疗中的作用是一个活跃的研究领域。
本综述重点介绍了尼拉帕利的药理学、临床疗效和不良反应，这些都通过前瞻性临床试验和已批准的适应证得到证实。
尼拉帕利的出现开创了 PARP 抑制剂的应用时代，无论生物标志物状态如何。最近的研究强调了需要更准确的生物标志物来识别最有可能从 PARP 抑制剂治疗中获益的患者。在未来 5 年内，我们预计将进一步扩大并阐明尼拉帕利在卵巢癌治疗中的最佳适应证。
