Pharmacokinetics and Bioequivalence Evaluation of 2 Formulations of Tenofovir Alafenamide
© 2021, The American College of Clinical Pharmacology..
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).
| Medienart: |
E-Artikel |
|---|
| Erscheinungsjahr: |
2021 |
|---|---|
| Erschienen: |
2021 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:10 |
|---|---|
| Enthalten in: |
Clinical pharmacology in drug development - 10(2021), 12 vom: 05. Dez., Seite 1519-1527 |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
Li, Zhihui [VerfasserIn] |
|---|
| Links: |
|---|
| Themen: |
99YXE507IL |
|---|
| Anmerkungen: |
Date Completed 04.04.2022 Date Revised 05.04.2022 published: Print-Electronic Citation Status MEDLINE |
|---|
| doi: |
10.1002/cpdd.985 |
|---|
| funding: |
|
|---|---|
| Förderinstitution / Projekttitel: |
|
| PPN (Katalog-ID): |
NLM32896459X |
|---|
| LEADER | 01000naa a22002652 4500 | ||
|---|---|---|---|
| 001 | NLM32896459X | ||
| 003 | DE-627 | ||
| 005 | 20231225204057.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 231225s2021 xx |||||o 00| ||eng c | ||
| 024 | 7 | |a 10.1002/cpdd.985 |2 doi | |
| 028 | 5 | 2 | |a pubmed24n1096.xml |
| 035 | |a (DE-627)NLM32896459X | ||
| 035 | |a (NLM)34352149 | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
| 041 | |a eng | ||
| 100 | 1 | |a Li, Zhihui |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Pharmacokinetics and Bioequivalence Evaluation of 2 Formulations of Tenofovir Alafenamide |
| 264 | 1 | |c 2021 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a ƒaComputermedien |b c |2 rdamedia | ||
| 338 | |a ƒa Online-Ressource |b cr |2 rdacarrier | ||
| 500 | |a Date Completed 04.04.2022 | ||
| 500 | |a Date Revised 05.04.2022 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a © 2021, The American College of Clinical Pharmacology. | ||
| 520 | |a 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) | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 4 | |a bioequivalence | |
| 650 | 4 | |a pharmacokinetics | |
| 650 | 4 | |a tenofovir alafenamide | |
| 650 | 7 | |a Tablets |2 NLM | |
| 650 | 7 | |a Tenofovir |2 NLM | |
| 650 | 7 | |a 99YXE507IL |2 NLM | |
| 650 | 7 | |a tenofovir alafenamide |2 NLM | |
| 650 | 7 | |a EL9943AG5J |2 NLM | |
| 650 | 7 | |a Alanine |2 NLM | |
| 650 | 7 | |a OF5P57N2ZX |2 NLM | |
| 700 | 1 | |a Liu, Jingyan |e verfasserin |4 aut | |
| 700 | 1 | |a Ju, Gehang |e verfasserin |4 aut | |
| 700 | 1 | |a Yan, Keyu |e verfasserin |4 aut | |
| 700 | 1 | |a Mao, Yong |e verfasserin |4 aut | |
| 700 | 1 | |a Liu, Qingchun |e verfasserin |4 aut | |
| 700 | 1 | |a Yang, Xinlu |e verfasserin |4 aut | |
| 700 | 1 | |a Zhang, Rong |e verfasserin |4 aut | |
| 700 | 1 | |a Qiu, Wen |e verfasserin |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t Clinical pharmacology in drug development |d 2012 |g 10(2021), 12 vom: 05. Dez., Seite 1519-1527 |w (DE-627)NLM250185032 |x 2160-7648 |7 nnns |
| 773 | 1 | 8 | |g volume:10 |g year:2021 |g number:12 |g day:05 |g month:12 |g pages:1519-1527 |
| 856 | 4 | 0 | |u http://dx.doi.org/10.1002/cpdd.985 |3 Volltext |
| 912 | |a GBV_USEFLAG_A | ||
| 912 | |a GBV_NLM | ||
| 951 | |a AR | ||
| 952 | |d 10 |j 2021 |e 12 |b 05 |c 12 |h 1519-1527 | ||