PARP抑制剂在肿瘤中的治疗现状及展望  

Current Status and Prospect of PARP Inhibitors in the Treatment of Tumors

作　　者：黄佳炎 尹香花[2] HUANG Jiayan;YIN Xianghua(Graduate School of Dalian Medical University,Dalian,Liaoning,116044,China;Department of Obstetrics and Gynecology,Northern Jiangsu People’s Hospital,Yangzhou,Jiangsu,225001,China)

机构地区：[1]大连医科大学研究生院,辽宁大连116044 [2]苏北人民医院妇产科,江苏扬州225001

出　　处：《肿瘤药学》2021年第3期300-304,314,共6页Anti-Tumor Pharmacy

摘　　要：聚ADP-核糖聚合酶(PARP)抑制剂是治疗具有同源重组缺陷(HRD)肿瘤的靶向药物,其利用合成致死原理,针对特定的DNA修复途径,诱导BRCA1/2突变的肿瘤合成杀伤。目前,4种PARP抑制剂(奥拉帕利、卢卡帕利、尼拉帕利和他拉唑帕利)已获得美国食品药品监督管理局(FDA)批准,用于卵巢癌、转移性乳腺癌、晚期前列腺癌和胰腺癌的治疗,尤其在BRCA1/2突变的患者获益中最多。本文综述了目前临床已知的PARP抑制剂的作用机制、应用现状、安全性及耐药性,并对其未来发展作一展望。Poly ADP-ribose polymerase(PARP)inhibitors are target drugs for the treatment of tumors with homologous recombination defects(HRD).They target specific DNA repair pathways and induce tumors with BRCA1/2 mutations to synthetic lethal interactions.Currently,four PARP inhibitors(Olaparib,Rucaparib,Niraparib and Talazoparib)have been approved by the US Food and Drug Administration(FDA)for the treatment of ovarian,metastatic breast,advanced prostate and pancreatic cancer,especially in patients with BRCA1/2 mutations.In this paper are reviewed the mechanism,application,safety and drug resistance of PARP inhibitors.The future development of PARP inhibitors is also prospected.

关 键 词：PARP抑制剂 BRCA突变 同源重组缺陷 耐药性 安全性 

分 类 号：R730.5[医药卫生—肿瘤]