Pharmacokinetics and Bioequivalence Evaluation of 2 Formulations of Tenofovir Alafenamide
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 (C max) 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 C max, 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 C max 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)..
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2021 |
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| Erschienen: |
2021 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:10 |
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| Enthalten in: |
Clinical Pharmacology in Drug Development - 10(2021), 12, Seite 1519-1527 |
| Beteiligte Personen: |
Li, Zhihui [VerfasserIn] |
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| BKL: |
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| Anmerkungen: |
© American College of Clinical Pharmacology |
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| Umfang: |
9 |
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| doi: |
10.1002/cpdd.985 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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WLY003866696 |
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| 520 | |a 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 (C max) 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 C max, 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 C max 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). | ||
| 700 | 1 | |a Liu, Jingyan |4 aut | |
| 700 | 1 | |a Ju, Gehang |4 aut | |
| 700 | 1 | |a Yan, Keyu |4 aut | |
| 700 | 1 | |a Mao, Yong |4 aut | |
| 700 | 1 | |a Liu, Qingchun |4 aut | |
| 700 | 1 | |a Yang, Xinlu |4 aut | |
| 700 | 1 | |a Zhang, Rong |4 aut | |
| 700 | 1 | |a Qiu, Wen |4 aut | |
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