Comparative pharmacokinetics between tenofovir disoproxil phosphate and tenofovir disoproxil fumarate in healthy subjects

• DOI: 10.12793/tcp.2021.29.e4
• Publication Date: 2021-03-31T04:36:42Z
• Authors: Sangmi Lee; Eunwoo Kim; Seol Ju Moon; Jina Jung; SeungHwan Lee; Kyung-Sang Yu
• Keywords: Bioequivalence; Tenofovir; Crossover study

Tenofovir is the representative treatment for human immunodeficiency virus and hepatitis B infection. This study was conducted to assess pharmacokinetics (PKs) safety characteristics after a single administration of tenofovir disoproxil phosphate compared fumarate in healthy male subjects. An open-label, randomized, administration, two-treatment, two-sequence crossover 37 volunteers. Serial blood samples were collected up 72 hours. Non-compartmental analysis used calculate PK parameters. The 90% confidence intervals (90% CIs) geometric mean ratio (GMR) calculated comparing fumarate. Safety assessments performed including clinical laboratory tests, adverse events, etc. during study. GMR CIs 1.0514 (0.9527-1.1603) Cmax 1.0375 (0.9516-1.1311) AUClast, respectively, both fell within conventional bioequivalence range 0.8-1.25. Both salt forms tolerable. demonstrated that (292 mg) bioequivalent (300 mg).