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

Yven Van Herrewege; Jo Michiels; Jens Van Roey; Katrien Fransen; Luc Kestens; Jan Balzarini; Paul Lewi; Guido Vanham; Paul Janssen

doi:10.1128/AAC.48.1.337-339.2004

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

Antimicrob Agents Chemother. 2004 Jan;48(1):337-9. doi: 10.1128/AAC.48.1.337-339.2004.

Authors

Yven Van Herrewege¹, Jo Michiels, Jens Van Roey, Katrien Fransen, Luc Kestens, Jan Balzarini, Paul Lewi, Guido Vanham, Paul Janssen

Affiliation

¹ Laboratory of Immunology, Institute of Tropical Medicine, Antwerp, Belgium. yvherrewege@itg.be

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Anilides / pharmacology*
Anti-HIV Agents / pharmacology*
CD4-Positive T-Lymphocytes / drug effects
CD4-Positive T-Lymphocytes / virology
Cell-Free System
Cells, Cultured
Coculture Techniques
Dendritic Cells / virology
Enzyme-Linked Immunosorbent Assay
Furans / pharmacology*
HIV Infections / prevention & control*
HIV Infections / virology
HIV-1
Humans
Pyrimidines / pharmacology
Reverse Transcriptase Inhibitors / pharmacology*
Thioamides

Substances

Anilides
Anti-HIV Agents
Furans
Pyrimidines
Reverse Transcriptase Inhibitors
Thioamides
UC-781
Dapivirine