Pharmacokinetics and Bioequivalence Evaluation of 2 Formulations of Tenofovir Alafenamide. Issue 12 (5th August 2021)

• Record Type: Journal Article
• Authors: Li, Zhihui; Liu, Jingyan; Ju, Gehang; Yan, Keyu; Mao, Yong; Liu, Qingchun; Yang, Xinlu; Zhang, Rong; Qiu, Wen
• Is Part Of: Clinical pharmacology in drug development. Volume 10:Issue 12(2021)
• Page Start: 1519
• Page End: 1527
• Publication Date: 2021-08-05
• Subjects: bioequivalence -- pharmacokinetics -- tenofovir alafenamide; Drugs -- Testing -- Periodicals; Drug development -- Periodicals; Clinical pharmacology -- Periodicals; 615.580724
• DOI: 10.1002/cpdd.985
• Languages: English
• ISSNs: 2160-7648

Abstract

Abstract: The study was conducted to compare the pharmacokinetics and safety profiles of 2 brands of tenofovir alafenamide (TAF) fumarate tablets. This research was a 2‐preparation, 2‐sequence, 4‐period crossover, completely replicated study in 68 healthy Chinese subjects under fasting and fed conditions. The mean values of the area under the concentration‐time curve from time 0 to the last time point with blood sample collection (AUC0‐t ), area under the concentration‐time curve from time 0 to infinity (AUC0‐∞ ), and maximum concentration (Cmax ) for the test and reference products of TAF were 248.5 and 275.7 ng/mL, 148.1 and 157.8 ng h/mL, and 148.4 and 158.1 ng h/mL, respectively, under the fasting condition. On the other hand, the mean value of Cmax, AUC0‐t, and AUC0‐∞ for the test and reference formulations of TAF were 244.6 and 246.7 ng/mL, 230.4 and 244.9 ng h/mL, and 233.2 and 246.2 ng h/mL, respectively, under the fed condition. The 90% confidence intervals for geometric mean ratios of AUC0–t and AUC0‐∞ of TAF in fasting and fed states were within the bioequivalence acceptance limits when tested using the average‐bioequivalence method. The point estimate value for geometric mean ratio of Cmax in fasting and fed states (88.4% and 95.5%, respectively) were within the bioequivalence acceptance limits as per the reference‐scaled average‐bioequivalence method. The safety profiles of the 2 formulations were comparable. Pharmacokinetic analysis demonstrated that the test formulations of TAF exhibited bioequivalence to the reference and were well tolerated by healthy Chinese subjects (Study Registry Identification Number: CTR20190086; CTR20190087).