Vicriviroc -: Anti-HIV agent viral entry inhibitor chemokine CCR5 antagonist

被引：1

作者：

Revill, P. ^{[1
]}

Bayes, M. ^{[1
]}

Bozzo, J. ^{[1
]}

Serradell, N. ^{[1
]}

Rosa, E. ^{[1
]}

Bolos, J. ^{[1
]}

机构：

[1] Univ Politecn Cataluna, E-08080 Barcelona, Spain

来源：

DRUGS OF THE FUTURE | 2007年 / 32卷 / 05期

关键词：

1-(4,6-Dimethylpyrimidin-5-yl)-1-[4-[4-[2-methoxy-1(R)-[4-(trifluoromethyl)phenyllethyll-3(S)-methylpiperazin-1-yl]-4-methylpiperidin-1; -yl]methanone; 5-[4-[4-[2-Methoxy-1(R)-[4-(trifluoromethyl)phenyllethyll-3(S)-methylpiperazin-1-yl]-4-methylpiperidin-1-ylcarbonyll-4,6dimethylpyrimidine;

D O I：

10.1358/dof.2007.032.05.1100315

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Vicriviroc is a viral entry inhibitor under development for the treatment of HIV-1 infection in combination with other antiretrovirals. It is a small-molecule antagonist of the chemokine receptor CCR5, which is expressed on the surface of macrophages and leukocytes and is required for the efficient entry of R5-tropic HIV into target cells. Vicriviroc has potent activity against a wide range of primary HIV-1 isolates and an excellent pharmacokinetic profile. In a phase II clinical trial, vicriviroc was associated with treatment failures in combination with the reverse transcriptase inhibitors lamivudine/zidovudine (Combivir (R)), whereas in another phase II trial, vicriviroc (10 mg once daily and above) was effective in reducing HIV viral load and increasing CD(4+) counts in combination with optimized background therapies containing ritonavir (which boosts the pharmacokinetics of vicriviroc) and a protease inhibitor.

引用

页码：417 / 427

页数：11