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<p>This study compared the pharmacokinetic bioequivalence and safety of a new free-base formulation of 25&#xa0;mg tenofovir alafenamide (TAF) to those of a reference formulation under fasting conditions. In this phase I, randomized, open-label, two-sequence, four-period, fully replicated crossover trial, 48 healthy volunteers were enrolled to receive single doses of the test and reference formulations in the T-R-T-R or R-T-R-T sequences. The plasma concentrations of TAF and tenofovir were measured and analyzed using non-compartmental methods. As the TAF concentration exhibits high intra-individual variability, reference-scaled average bioequivalence can be applied. The safety and tolerability were monitored during the study. All 48 volunteers received the study drug at least once. The pharmacokinetic analysis included 44 and 46 volunteers for TAF and tenofovir, respectively. The intra-individual coefficient of variation for the plasma maximum concentration (C<sub>max</sub>) of the reference TAF formulation was 59.86%, permitting an expanded acceptance range of 0.6984–1.4319. Both TAF and tenofovir met the bioequivalence criteria as the geometric mean ratios (test/reference) and 90% confidence intervals for the C<sub>max</sub> and AUC<sub>last</sub> of each substance were within 0.80–1.25. Both formulations were safe and well-tolerated, and no serious adverse events were observed. The novel free-base formulation of 25&#xa0;mg TAF demonstrated pharmacokinetic bioequivalence with the reference formulation and was safe for use in healthy volunteers.</p>

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Pharmacokinetics and safety of a new free-base formulation of tenofovir alafenamide 25 mg in healthy volunteers: a randomized, open-label, four-period, fully replicated crossover bioequivalence study

  • 期刊论文

  • 发表日期：

    2026年5月9日

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  • Eunwoo Kim,
  • Wonsuk Shin,
  • Hyounggyoon Yoo,
  • Yilseob Lee,
  • Kwang Hyun Ahn,
  • Anhye Kim

摘要

This study compared the pharmacokinetic bioequivalence and safety of a new free-base formulation of 25 mg tenofovir alafenamide (TAF) to those of a reference formulation under fasting conditions. In this phase I, randomized, open-label, two-sequence, four-period, fully replicated crossover trial, 48 healthy volunteers were enrolled to receive single doses of the test and reference formulations in the T-R-T-R or R-T-R-T sequences. The plasma concentrations of TAF and tenofovir were measured and analyzed using non-compartmental methods. As the TAF concentration exhibits high intra-individual variability, reference-scaled average bioequivalence can be applied. The safety and tolerability were monitored during the study. All 48 volunteers received the study drug at least once. The pharmacokinetic analysis included 44 and 46 volunteers for TAF and tenofovir, respectively. The intra-individual coefficient of variation for the plasma maximum concentration (Cmax) of the reference TAF formulation was 59.86%, permitting an expanded acceptance range of 0.6984–1.4319. Both TAF and tenofovir met the bioequivalence criteria as the geometric mean ratios (test/reference) and 90% confidence intervals for the Cmax and AUClast of each substance were within 0.80–1.25. Both formulations were safe and well-tolerated, and no serious adverse events were observed. The novel free-base formulation of 25 mg TAF demonstrated pharmacokinetic bioequivalence with the reference formulation and was safe for use in healthy volunteers.