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.
Yven Van Herrewege  1 ,  Jo Michiels ,  Jens Van Roey ,  Katrien Fransen ,  Luc Kestens ,  Jan Balzarini ,  Paul Lewi ,  Guido Vanham ,  Paul Janssen
Affiliations
  • 1. Laboratory of Immunology, Institute of Tropical Medicine, Antwerp, Belgium. [email protected]
PMID: 14693562 DOI: 10.1128/AAC.48.1.337-339.2004
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.

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