176161-24-3
176161-24-3 结构式
基本信息
苯并咪唑核苷
BENZIMIDAVIR 苯并咪唑核苷
Maribavi
Maribavir
BW 1263W94
GW 257406X
BENZIMIDAVIR
5,6-DICHLORO-2-ISOPROPYLAMINO-1-(-L-RIBOFURANOSYL)-LH-BENZIMIDAZOLE
5,6-DICHLORO-2-(ISOPROPYLAMINO)-1-(BETA-L-RIBOFURANOSYL)-1H-BENZIMIDAZOLE
1H-Benzimidazol-2-amine, 5,6-dichloro-N-(1-methylethyl)-1-β-L-ribofuranosyl-
5,6-Dichloro-N-(1-methylethyl)-1-beta-L-ribofuranosyl-1H-benzimidazol-2-amine
物理化学性质
常见问题列表
马立巴韦（Maribavir）是一种新的苯并咪唑核糖苷类药物，属于pUL97蛋白激酶抑制剂，对CMV具有独特的作用机制。马立巴韦的口服吸收率高而不良反应较少，具有较好的临床安全性。马立巴韦最初由密歇根大学开发，而后授权给葛兰素史克制药。目前马立巴韦分别由葛兰素史克制药、Shire Pharmaceuticals 和武田制药在全球多个国家和地区进行Ⅲ期临床试验。
HCMV
Maribavir is a potent inhibitor of the autophosporylation of the wild type and all the major Ganciclovir (GCV) resistant UL97 mutants analysed with a mean IC 50 of 35 nM. The M460I mutation results in hypersensitivity to Maribavir with an IC 50 of 4.8 nM. A Maribavir resistant mutant of UL97 (L397R) is functionally compromised as both a Ganciclovir kinase and a protein kinase (~ 10% of wild type levels). Enzyme kinetic experiments demonstrate that Maribavir is a competitive inhibitor of ATP with a K i of 10 nM. Maribavir (1263W94) inhibits viral replication in a dose-dependent manner, with IC 50 of 0.12±0.01 μM as measured by a multicycle DNA hybridization assay. The pUL97 protein kinase is strongly inhibited by Maribavir, with 50% inhibition occurring at 3 nM.