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芦卡帕利:卵巢癌治疗药物。

Rucaparib: A Review in Ovarian Cancer.

机构信息

Springer, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand.

出版信息

Target Oncol. 2019 Apr;14(2):237-246. doi: 10.1007/s11523-019-00629-5.

Abstract

Rucaparib (Rubraca) is a small molecule poly(ADP-ribose) polymerase (PARP) inhibitor with potent activity against PARP-1, -2 and -3. It is approved in the USA and the EU for the treatment of adult patients with BRCA-mutated ovarian cancer who have been treated with two or more lines of chemotherapy. Rucaparib is also approved in the USA and the EU for use as maintenance therapy in adult patients with recurrent or relapsed ovarian cancer who are in a complete or partial response to platinum-based chemotherapy. Based on an analysis of patients across two phase II clinical trials, rucaparib displayed clinical activity as third- (or later-) line treatment of BRCA-mutated ovarian cancer, with rucaparib-treated patients having a confirmed objective response rate of 54%. Furthermore, as demonstrated in the randomized, placebo-controlled, phase III ARIEL3 trial, rucaparib significantly improved progression-free survival when used as maintenance treatment in patients with platinum-sensitive ovarian cancer. Rucaparib had an acceptable tolerability profile in clinical trials in women with ovarian cancer. Common adverse events were generally manageable with dose modification and/or supportive care. Thus, currently available data indicate that rucaparib is a useful addition to the options available to clinicians for the treatment of advanced ovarian cancer, in both the treatment and maintenance therapy settings.

摘要

鲁卡帕尼(Rubraca)是一种小分子聚(ADP-核糖)聚合酶(PARP)抑制剂,对 PARP-1、-2 和 -3 具有很强的抑制作用。它在美国和欧盟被批准用于治疗接受过两线或以上化疗的 BRCA 突变型卵巢癌成年患者。鲁卡帕尼还在美国和欧盟被批准用于对铂类化疗有完全或部分反应的复发性或持续性卵巢癌成年患者的维持治疗。基于两项 II 期临床试验的患者分析,鲁卡帕尼作为 BRCA 突变型卵巢癌的三线(或更后线)治疗显示出临床疗效,接受鲁卡帕尼治疗的患者的确认客观缓解率为 54%。此外,在随机、安慰剂对照的 III 期 ARIEL3 试验中,鲁卡帕尼作为铂类敏感卵巢癌的维持治疗显著改善了无进展生存期。在卵巢癌女性的临床试验中,鲁卡帕尼具有可接受的耐受性。常见的不良反应通常可以通过剂量调整和/或支持性护理来控制。因此,目前的数据表明,鲁卡帕尼是治疗晚期卵巢癌的临床医生的治疗选择的有益补充,包括治疗和维持治疗环境。

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