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Pharmacokinetic Evaluation of Emtricitabine in Combination With Other Nucleoside Antivirals in Healthy Volunteers
Author(s) -
Zong Jian,
Chittick Gregory E.,
Wang Laurene H.,
Hui James,
Begley John A.,
Blum M. Robert
Publication year - 2007
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/0091270007300808
Subject(s) - emtricitabine , pharmacokinetics , pharmacology , zidovudine , stavudine , lamivudine , medicine , nucleoside , drug , reverse transcriptase inhibitor , chemistry , human immunodeficiency virus (hiv) , virology , antiretroviral therapy , virus , viral load , biochemistry , hepatitis b virus , viral disease
Emtricitabine is a potent nucleoside reverse transcriptase inhibitor approved as a once‐daily drug in combination with other antiretroviral agents for the treatment of HIV infection. Several phase I studies were conducted in healthy volunteers over the course of clinical development to evaluate whether pharmacokinetic drug—drug interactions exist between emtricitabine and other nucleoside antivirals that are extensively eliminated by renal excretion. Potential interactions with stavudine and famciclovir were evaluated in single‐dose studies, whereas interactions with zidovudine and its major metabolite, zidovudine glucuronide, were evaluated in a multiple‐dose study. Plasma pharmacokinetic profiles and, in some studies, urinary excretion data were evaluated when each drug was administered alone and in combination with emtricitabine. Safety and plasma pharmacokinetic profiles of each drug administered alone or with emtricitabine were consistent with historical data. Statistical analyses indicated that there were no significant interactions between emtricitabine and these 3 nucleoside antivirals.