In vitro evaluation of nonnucleoside reverse transcriptase inhibitors UC-781 and TMC120-R147681 as human immunodeficiency virus microbicides

被引:124
作者
Van Herrewege, Y
Michiels, J
Van Roey, J
Fransen, K
Kestens, L
Balzarini, J
Lewi, P
Vanham, G
Janssen, P
机构
[1] Inst Trop Med, Dept Microbiol, Immunol Lab, B-2000 Antwerp, Belgium
[2] Inst Trop Med, Dept Microbiol, AIDS Reference Lab, B-2000 Antwerp, Belgium
[3] Tibotec Virco NV, Mechelen, Belgium
[4] Katholieke Univ Leuven, Rega Inst Med Res, Lab Virol & Chemotherapy, B-3000 Louvain, Belgium
[5] Janssen Pharmaceut, Ctr Mol Design, Vosselaar, Belgium
关键词
D O I
10.1128/AAC.48.1.337-339.2004
中图分类号
Q93 [微生物学];
学科分类号
071005 ; 100705 ;
摘要
The nonnucleoside reverse transcriptase inhibitors UC-781 and TMC120-R147681 (Dapivirine) effectively prevented human immunodeficiency virus (HIV) infection in cocultures of monocyte-derived dendritic cells and T cells, representing primary targets in sexual transmission. Both drugs had a favorable therapeutic index. A 24-h treatment with 1,000 nM UC-781 or 100 nM TMC120-R147681 prevented cell-free HIV infection, whereas 10-fold-higher concentrations blocked cell-associated HIV.
引用
收藏
页码:337 / 339
页数:3
相关论文
共 22 条
[21]   Sexual transmission of HIV: infectiousness and prevention [J].
Vernazza, PL ;
Eron, JJ ;
Fiscus, SA ;
Cohen, MS .
AIDS, 1999, 13 (02) :155-166
[22]   Human immunodeficiency virus type I in the semen of men receiving highly active antiretroviral therapy [J].
Zhang, H ;
Dornadula, G ;
Beumont, M ;
Livornese, L ;
Van Uitert, B ;
Henning, K ;
Pomerantz, RJ .
NEW ENGLAND JOURNAL OF MEDICINE, 1998, 339 (25) :1803-1809