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Antimicrobial Agents and Chemotherapy, January 2004, p. 337-339, Vol. 48, No. 1
0066-4804/04/$08.00+0     DOI: 10.1128/AAC.48.1.337-339.2004
Copyright © 2004, American Society for Microbiology. All Rights Reserved.

In Vitro Evaluation of Nonnucleoside Reverse Transcriptase Inhibitors UC-781 and TMC120-R147681 as Human Immunodeficiency Virus Microbicides{dagger}

Yven Van Herrewege,1* Jo Michiels,1 Jens Van Roey,2 Katrien Fransen,3 Luc Kestens,1 Jan Balzarini,4 Paul Lewi,5 Guido Vanham,1 and Paul Janssen5

Laboratory of Immunology,1 AIDS Reference Laboratory, Department of Microbiology, Institute of Tropical Medicine, Antwerp,3 Tibotec-Virco NV, Mechlin,2 Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, Leuven,4 Center for Molecular Design, Janssen Pharmaceutica, Vosselaar, Belgium5

Received 11 June 2003/ Returned for modification 26 August 2003/ Accepted 23 September 2003

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.

* Corresponding author. Mailing address: Laboratory of Immunology, Institute of Tropical Medicine; 155 Nationalestraat, B-2000 Antwerp, Belgium. Phone: 32-3-247.62.26. Fax: 32-3-247.62.31. E-mail: yvherrewege{at}itg.be.

{dagger} This work is dedicated to the memory of Paul A. J. Janssen, founder of Janssen Pharmaceutica and the Center for Molecular Design.

Antimicrobial Agents and Chemotherapy, January 2004, p. 337-339, Vol. 48, No. 1
0066-4804/04/$08.00+0     DOI: 10.1128/AAC.48.1.337-339.2004
Copyright © 2004, American Society for Microbiology. All Rights Reserved.



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