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TAF Potency vs TDF-Resistant Virus - Limited Evolution of Tenofovir-Resistant Viruses after Extended TAF Resistance Selection
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Reported by Jules Levin
International Workshop on Antiviral Drug Resistance
June 3-7, 2014 Berlin, Germany
NA Margot, RR Ram, MD Miller, C Callebaut
Gilead Sciences Inc, Foster City, CA, United States
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Sitges/2012: Resistance and Potency of GS-7340, a Next-Generation Tenofovir Prodrug (06/15/12)
GS-7340 showed superior antiviral potency to TDF in the presence of human serum, consistent with the higher intracellular TFV-DP levels and greater antiviral activity seen clinically at significantly lower doses than TDF. GS-7340 selected K65R in RT after extended in vitro resistance selection....The higher intracellular TFV-DP levels achieved with GS-7340 may enable activity against previously defined TDF-resistant isolates
........GS-7340 antiviral activity was evaluated in PBMCs against a panel of wild-type (WT) and drug-resistant HIV-1 clinical isolates, using RT monitoring and reference antiretroviral drugs. GS-7340 resistance profile was characterized against a panel of NRTI-resistant patient-derived viruses using the PhenoSense™ Assay (Monogram Biosciences)
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