Human Sulfotransferase 1A1-Dependent Mutagenicity of 12-Hydroxy-nevirapine: The Missing Link?

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Abstract

Nevirapine (NVP) is a frequently used anti-HIV drug. Despite its efficacy, NVP has been associated with serious skin and liver injuries in exposed patients and with increased incidences of hepatoneoplasias in rodents. Current evidence supports the involvement of reactive metabolites in the skin and liver toxicities of NVP, formed by cytochrome P450-mediated oxidations and/or subsequent phase II sulfonation. However, to date, standard in vitro genotoxicity tests have provided no evidence that NVP is either mutagenic or clastogenic. The human sulfotransferase 1A1-dependent mutagenidty of 12-hydroxy-NVP, one of the major metabolites of NVP, is demonstrated here.
Original languageEnglish
Pages (from-to)1967-1971
Number of pages5
JournalChemical Research In Toxicology
Volume27
Issue number11
DOIs
Publication statusPublished - 2014

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