Institute of Tropical Medicine Antwerp
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Reverse transcriptase inhibitors as microbicides

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Show simple item record Lewi, P. Heeres, J. Ariën, K. Venkatraj, M. Joossens, J. Van der Veken, P. Augustyns, K. Vanham, G. 2012-02-29T14:08:58Z 2012-02-29T14:08:58Z 2012
dc.identifier.issn 1570-162X
dc.identifier.other ITG-B3A
dc.identifier.other ITG-BLA
dc.identifier.other DBM
dc.identifier.other U-VIROL
dc.identifier.other JIF
dc.identifier.other UPD43
dc.description.abstract The CAPRISA 004 study in South Africa has accelerated the development of vaginal and rectal microbicides containing antiretrovirals that target specific enzymes in the reproduction cycle of HIV, especially reverse transcriptase inhibitors (RTI). In this review we discuss the potential relevance of HIV-1 RTIs as microbicides, focusing in the nucleotide RTI tenofovir and six classes of nonnucleoside RTIs (including dapivirine, UC781, urea and thiourea PETTs, DABOs and a pyrimidinedione). Although tenofovir and dapivirine appear to be most advanced in clinical trials as potential microbicides, several issues remain unresolved, e.g., the importance of nonhuman primates as a "gatekeeper" for clinical trials, the emergence and spread of drug-resistant mutants, the combination of microbicides that target different phases of viral reproduction and the accessibility to microbicides in low-income countries. Thus, here we discuss the latest research on RTI as microbicides in the light of the continuing spread of the HIV pandemic from the point of view of medicinal chemistry, virological, and pharmaceutical studies. en
dc.language English en
dc.subject Viral diseases en
dc.subject HIV en
dc.subject AIDS en
dc.subject Disease transmission, sexual en
dc.subject Transmission interruption en
dc.subject Microbicides en
dc.subject Development en
dc.subject Reverse transcriptase inhibitors en
dc.subject Vaginal gel en
dc.subject Nucleotides en
dc.subject Tenofovir en
dc.subject Clinical trials en
dc.subject Non-nucleoside en
dc.subject Review of the literature en
dc.title Reverse transcriptase inhibitors as microbicides en
dc.type Article en
dc.citation.issue 1 en
dc.citation.jtitle Current HIV Research en
dc.citation.volume 10 en
dc.citation.pages 27-35 en
dc.citation.jabbreviation Curr HIV Res en

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