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Rucaparib是由Clovis公司研发的一种新的聚腺苷二磷酸核糖聚合酶抑制剂,2016年12月FDA批准其作为单一疗法用于治疗经过两线或两线以上化疗且伴有BRCA基因突变相关的晚期卵巢癌。在两项单臂临床试验中,患者对该药的总应答率超过50%,其上市为卵巢癌患者带来了新的治疗选择。市场预测Rucaparib的年销售额有望超过13亿美元。笔者对其基本性质、作用机制、药代动力学、药物相互作用、临床研究、不良反应及研发现状等方面做一综述。
Rucaparib is a new poly (ADP-ribose) polymerase inhibitor developed by Clovis and approved by the FDA in December 2016 as a monotherapy for the treatment of patients with two or more lines of chemotherapy associated with BRCA mutations Advanced ovarian cancer. In two one-arm clinical trials, patients had a total response rate of over 50% to this drug, and the introduction of a new treatment option for patients with ovarian cancer. Market Forecast Rucaparib’s annual sales are expected to exceed 1.3 billion US dollars. The author summarizes its basic properties, mechanism of action, pharmacokinetics, drug interactions, clinical studies, adverse reactions and the status of research and development.