What question did this study set out to answer?

Characterize the pharmacokinetic and pharmacodynamic profiles of emtricitabine to establish the pharmacological basis for a once-daily dosing schedule in HIV infection.

November 1, 2004AIDS Research and Human Retroviruses

Pharmacokinetic and Pharmacodynamic Characteristics of Emtricitabine Support Its Once Daily Dosing for the Treatment of HIV Infection

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Characterize the pharmacokinetic and pharmacodynamic profiles of emtricitabine to establish the pharmacological basis for a once-daily dosing schedule in HIV infection.
Conducted a 14-day, open-label monotherapy trial in therapy-naive HIV-infected subjects evaluating doses of 25, 100, and 200 mg administered once or twice daily.
Measured serial concentrations of plasma HIV RNA, plasma emtricitabine, and intracellular peripheral blood mononuclear cell (PBMC) FTC-5'-triphosphate (FTC-5'-TP).
Supplemented findings with steady-state pharmacokinetic trials in healthy volunteers and HIV-infected patients receiving 200 mg emtricitabine once daily.
Plasma emtricitabine exhibited an elimination half-life of 8–10 hours, whereas active intracellular PBMC FTC-5'-TP demonstrated a prolonged half-life of 39 hours.
Suppression of plasma HIV RNA strongly correlated with intracellular FTC-5'-TP concentrations.
Both intracellular FTC-5'-TP accumulation and viral RNA suppression plateaued at daily emtricitabine doses of 200 mg or greater.

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Implication

Open-label monotherapy trial demonstrates sustained intracellular half-life and viral suppression in HIV-infected subjects, highlighting the viability of once-daily dosing.

Cite This Study

Wang et al. (2004) studied this question.

synapsesocial.com/papers/6a892569353a6a8ef2a5f77b https://doi.org/10.1089/0889222042544965

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Implication

Open-label monotherapy trial demonstrates sustained intracellular half-life and viral suppression in HIV-infected subjects, highlighting the viability of once-daily dosing.

Pharmacokinetic and Pharmacodynamic Characteristics of Emtricitabine Support Its Once Daily Dosing for the Treatment of HIV Infection

Key Points

Discussion

Implication

Cite This Study

Pharmacokinetic and Pharmacodynamic Characteristics of Emtricitabine Support Its Once Daily Dosing for the Treatment of HIV Infection

Key Points

Discussion

Implication

Cite This Study

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