[关键词]
[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(poly ADP-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。
[Key word]
[Abstract]
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.
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