Tenofovir Disoproxilfumarate is an antiviral drug. Pharmacokinetics The pharmacokinetics of tenofovir disoproxil fumarate have been evaluated in healthy volunteers and HIV-1 infected individuals. Tenofovir pharmacokinetics are similar between these populations.
Tenofovir is a water soluble diester prodrug of the active ingredient tenofovir. The oral bioavailability of tenofovir from Tenofovir in fasted subjects is approximately 25%. The pharmacokinetics of tenofovir are dose proportional over a Tenofovir dose range of 75 to 600 mg and are not affected by repeated dosing. DistributionIn vitro binding of tenofovir to human plasma or serum proteins is less than 0.7 and 7.2%, respectively, over the tenofovir concentration range 0.01 to 25 μg/mL. The volume of distribution at steady-state is 1.3 ± 0.6 L/kg and 1.2 ± 0.4 L/kg, following intravenous administration of tenofovir 1.0 mg/kg and 3.0 mg/kg.Metabolism and EliminationIn vitro studies indicate that neither tenofovir disoproxil nor tenofovir are substrates of CYP enzymes.