新型PARP抑制剂veliparib  

Novel PARP inhibitor—veliparib

作　　者：徐春秀[1,2] 石玉[2] 张师愚[1] 刘日[1,2] 李靖[3] 周祥[4] 邹美香[2] 李祎亮[2] 

机构地区：[1]天津中医药大学,天津300193 [2]天津药物研究院天津市新药设计与发现重点实验室,天津300193 [3]中国矿业大学,江苏徐州221116 [4]广西中医药大学,广西南宁530001

出　　处：《现代药物与临床》2013年第1期69-73,共5页Drugs & Clinic

摘　　要：肿瘤细胞能够激活自身DNA的损伤修复机制进行修复,从而导致其对抗肿瘤药物和放疗产生耐药性,而聚腺苷酸二磷酸核糖转移酶(polyADP-ribose polymerase,PARP)是一种DNA修复酶,在DNA修复通路中起关键作用。veliparib是一种新型高选择抑制PARP的苯并咪唑类化合物,体内外实验表明本品具有显著的抑制PARP活性的作用。在治疗转移性乳腺癌、结肠癌、转移性黑色素瘤和脑肿瘤方面已取得显著的效果,其与替莫唑胺联用治疗乳腺癌的研究即将进入III期临床。Tumor cells are able to activate their own DNA damage repair so as to repaire themselves,thus causing drug resistance against antitumor drugs and radiotherapy.While polyadenylation diphosphate ribose transferase （poly ADP-ribose polymerase,PARP） is a DNA repair enzyme which plays a key role in DNA repair pathways.Veliparib is a novel oral benzimidazole derivative that is a highly potent and selective PARP.The in vivo and in vitro experiments show that veliparib has a significant inhibition on PARP activity.In the treatment of metastatic breast cancer,colon cancer,metastatic melanoma,and brain tumor,the compound has made a significant effect,and its combination with temozolomide is going to enter phase Ⅲ in clinic for the treatment of breast cancer.

关 键 词：veliparib PARP抑制剂 抗肿瘤 

分 类 号：R91[医药卫生—药学]