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Target Oncol. 2018 Dec;13(6):801-808. doi: 10.1007/s11523-018-0606-x.
Olaparib (Lynparza®), a first-in-class poly (ADP-ribose) polymerase (PARP) inhibitor, has recently been approved in a new tablet formulation as maintenance treatment for recurrent high-grade epithelial ovarian, fallopian tube, or primary peritoneal cancer in patients who are in complete or partial response to platinum-based chemotherapy. Relative to an earlier capsule formulation, the tablet formulation of olaparib has improved bioavailability, thereby reducing pill burden and offering a more convenient dosage regimen. In the phase III SOLO2 study, maintenance treatment with olaparib tablets significantly prolonged median PFS (primary endpoint) relative to placebo in patients with platinum-sensitive, recurrent, ovarian cancer bearing gBRCA mutations. Results from an earlier phase II study (Study 19) assessing the capsule formulation supported these findings, with a significant PFS benefit (primary endpoint) observed with olaparib relative to placebo as maintenance therapy in patients with platinum-sensitive, recurrent, ovarian cancer, with or without BRCA mutations. Olaparib tablet had a manageable tolerability profile, with most adverse events of mild or moderate severity. Given its efficacy and manageable tolerability profile, olaparib tablets provide a useful maintenance treatment option for recurrent, platinum-sensitive ovarian cancer, regardless of BRCA mutation status, with the tablet formulation providing a more convenient dosing option.
奥拉帕利(Lynparza®),一种首创的多聚(ADP-核糖)聚合酶(PARP)抑制剂,最近以新的片剂制剂获批,用于对铂类化疗有完全或部分反应的复发性高级别上皮性卵巢癌、输卵管癌或原发性腹膜癌患者的维持治疗。与早期的胶囊制剂相比,奥拉帕利的片剂制剂具有改善的生物利用度,从而降低了药丸负担并提供了更方便的剂量方案。在 III 期 SOLO2 研究中,与安慰剂相比,奥拉帕利片剂维持治疗显著延长了携带 gBRCA 突变的铂敏感复发性卵巢癌患者的中位无进展生存期(主要终点)。评估胶囊制剂的早期 II 期研究(研究 19)的结果支持了这些发现,与安慰剂相比,奥拉帕利作为铂敏感、复发性卵巢癌患者的维持治疗具有显著的无进展生存期获益(主要终点),无论是否存在 BRCA 突变。奥拉帕利片剂具有可管理的耐受性特征,大多数不良事件为轻度或中度严重程度。鉴于其疗效和可管理的耐受性特征,奥拉帕利片剂为复发性铂敏感卵巢癌提供了一种有用的维持治疗选择,无论 BRCA 突变状态如何,片剂制剂提供了更方便的给药选择。