In vitro evaluation of nonnucleoside reverse transcriptase inhibitors UC-781 and TMC120-R147681 as human immunodeficiency virus microbicides
Van Herrewege, Y.; Michiels, J.; Van Roey, J.; Fransen, K.; Kestens, L.; Balzarini, J.; Lewi, P.; Vanham, G.; Janssen, P.
Antimicrobial Agents and ChemoTherapy 48(1): 337-339
2004
ISSN/ISBN: 0066-4804 PMID: 14693562 DOI: 10.1128/aac.48.1.337-339.2004Document Number: 258484
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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