Guney Eskiler G
Department of Medical Biology, Faculty of Medicine, Sakarya University, Sakarya, Turkey.
Drugs Today (Barc). 2019 Jul;55(7):459-467. doi: 10.1358/dot.2019.55.7.3015642.
Talazoparib tosylate (BMN-673, Talzenna; Pfizer) is an oral poly [ADP-ribose] polymerase (PARP) inhibitor (PARPi) that has been approved by the U.S. Food and Drug Administration (FDA) and the European Medicines Agency (EMA) for the treatment of germline BRCA-mutated locally advanced or metastatic breast cancer (BC). In preclinical and clinical studies, talazoparib exerted superior efficacy and offered a significant clinical benefit in advanced or metastatic BC patients harboring germline BRCA mutations compared with other PARPi and standard chemotherapy regimens through the concept of synthetic lethality. Thus, this review provides insight into the results of preclinical and clinical studies, highlights the current challenges of talazoparib and suggests innovative approaches to further improve its clinical efficacy and expand the use of talazoparib in advanced BC and/or triple-negative BC treatments beyond BRCA mutations.
甲苯磺酸他拉唑帕利(BMN-673,Talzenna;辉瑞公司)是一种口服聚[ADP-核糖]聚合酶(PARP)抑制剂(PARPi),已获得美国食品药品监督管理局(FDA)和欧洲药品管理局(EMA)批准,用于治疗种系BRCA突变的局部晚期或转移性乳腺癌(BC)。在临床前和临床研究中,通过合成致死性概念,与其他PARPi和标准化疗方案相比,他拉唑帕利在携带种系BRCA突变的晚期或转移性BC患者中显示出卓越的疗效,并提供了显著的临床益处。因此,本综述深入探讨了临床前和临床研究结果,突出了他拉唑帕利当前面临的挑战,并提出了创新方法,以进一步提高其临床疗效,并扩大他拉唑帕利在晚期BC和/或三阴性BC治疗中超出BRCA突变的应用。