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TAF versus TDF in hiv drugs

Joseph M Custodio, Susan K Chuck, Hoa Chu, Huyen Cao, Grace Ma, John Flaherty, John Ling, Brian P Kearney
The drug-drug interaction (DDI) potential between the fixed-dose combinations of ledipasvir/sofosbuvir 90/400 mg for hepatitis C virus and emtricitabine/rilpivirine/tenofovir alafenamide (TAF) 200/25/25 mg for HIV was evaluated in a randomized, open-label, single-center, multiple-dose, 3-way, 6-sequence, crossover Phase 1 study in 42 healthy subjects. Emtricitabine/rilpivirine/TAF had no relevant effect on the pharmacokinetic parameters of maximum concentration [Cmax ] and area under the concentration versus time curve over the dosing interval [AUCtau ] for ledipasvir, sofosbuvir, and the metabolites GS-566500 and GS-331007...
October 2017: Pharmacology Research & Perspectives
Nicolas A Margot, Audun Johnson, Michael D Miller, Christian Callebaut
Tenofovir alafenamide (TAF) is an investigational prodrug of the HIV-1 nucleotide reverse transcriptase (RT) inhibitor (NtRTI) tenofovir (TFV), with improved potency and drug delivery properties over the current prodrug, tenofovir disoproxil fumarate (TDF). TAF is currently in phase 3 clinical studies for the treatment of HIV-1 infection, in combination with other antiretroviral agents. Phase 1 and 2 studies have shown that TAF was associated with increased peripheral blood mononuclear cell (PBMC) drug loading and increased suppression of HIV-1 replication compared to treatment with TDF...
October 2015: Antimicrobial Agents and Chemotherapy
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