Cargando…
Pharmacokinetics and safety of Enasidenib following single oral doses in Japanese and Caucasian subjects
The aim of this study was to assess and compare the pharmacokinetics (PK) and safety of Enasidenib in healthy adult male Japanese subjects to healthy adult male Caucasian subjects. This was a phase 1, single dose study to evaluate the PK and safety of Enasidenib in healthy adult male Japanese subjec...
Autores principales: | , , , , , , |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
John Wiley and Sons Inc.
2018
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6199364/ https://www.ncbi.nlm.nih.gov/pubmed/30386625 http://dx.doi.org/10.1002/prp2.436 |
_version_ | 1783365130376970240 |
---|---|
author | Li, Yan Liu, Liangang Gomez, Diana Chen, Jian Tong, Zeen Palmisano, Maria Zhou, Simon |
author_facet | Li, Yan Liu, Liangang Gomez, Diana Chen, Jian Tong, Zeen Palmisano, Maria Zhou, Simon |
author_sort | Li, Yan |
collection | PubMed |
description | The aim of this study was to assess and compare the pharmacokinetics (PK) and safety of Enasidenib in healthy adult male Japanese subjects to healthy adult male Caucasian subjects. This was a phase 1, single dose study to evaluate the PK and safety of Enasidenib in healthy adult male Japanese subjects relative to healthy adult male Caucasian subjects. A total of 62 subjects (31 Japanese and 31 Caucasian) were enrolled into three dose cohorts (single doses of 50 mg, 100 mg, or 300 mg Enasidenib). Blood samples for PK assessment were collected up to 672 hours postdose. Safety was evaluated throughout the study. In the present study, we found that PK exposures of Enasidenib and its metabolite AGI‐16903 for Caucasian and Japanese subjects were comparable at the 50, 100, and 300 mg dose levels, demonstrated by that the 90% confidence intervals (CIs) of geometric mean ratios for AUCs and C (max) between these two populations generally contained 100% from all three treatment cohorts. In conclusion, PK exposures of Enasidenib and its metabolite AGI‐16903 for Caucasians and Japanese subjects were comparable and Enasidenib was safe and well tolerated with no apparent differences between Japanese and Caucasian subjects when administered as single oral doses of 50 mg, 100 mg, and 300 mg. |
format | Online Article Text |
id | pubmed-6199364 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | John Wiley and Sons Inc. |
record_format | MEDLINE/PubMed |
spelling | pubmed-61993642018-10-31 Pharmacokinetics and safety of Enasidenib following single oral doses in Japanese and Caucasian subjects Li, Yan Liu, Liangang Gomez, Diana Chen, Jian Tong, Zeen Palmisano, Maria Zhou, Simon Pharmacol Res Perspect Original Articles The aim of this study was to assess and compare the pharmacokinetics (PK) and safety of Enasidenib in healthy adult male Japanese subjects to healthy adult male Caucasian subjects. This was a phase 1, single dose study to evaluate the PK and safety of Enasidenib in healthy adult male Japanese subjects relative to healthy adult male Caucasian subjects. A total of 62 subjects (31 Japanese and 31 Caucasian) were enrolled into three dose cohorts (single doses of 50 mg, 100 mg, or 300 mg Enasidenib). Blood samples for PK assessment were collected up to 672 hours postdose. Safety was evaluated throughout the study. In the present study, we found that PK exposures of Enasidenib and its metabolite AGI‐16903 for Caucasian and Japanese subjects were comparable at the 50, 100, and 300 mg dose levels, demonstrated by that the 90% confidence intervals (CIs) of geometric mean ratios for AUCs and C (max) between these two populations generally contained 100% from all three treatment cohorts. In conclusion, PK exposures of Enasidenib and its metabolite AGI‐16903 for Caucasians and Japanese subjects were comparable and Enasidenib was safe and well tolerated with no apparent differences between Japanese and Caucasian subjects when administered as single oral doses of 50 mg, 100 mg, and 300 mg. John Wiley and Sons Inc. 2018-10-23 /pmc/articles/PMC6199364/ /pubmed/30386625 http://dx.doi.org/10.1002/prp2.436 Text en © 2018 The Authors. Pharmacology Research & Perspectives published by John Wiley & Sons Ltd, British Pharmacological Society and American Society for Pharmacology and Experimental Therapeutics. This is an open access article under the terms of the http://creativecommons.org/licenses/by-nc-nd/4.0/ License, which permits use and distribution in any medium, provided the original work is properly cited, the use is non‐commercial and no modifications or adaptations are made. |
spellingShingle | Original Articles Li, Yan Liu, Liangang Gomez, Diana Chen, Jian Tong, Zeen Palmisano, Maria Zhou, Simon Pharmacokinetics and safety of Enasidenib following single oral doses in Japanese and Caucasian subjects |
title | Pharmacokinetics and safety of Enasidenib following single oral doses in Japanese and Caucasian subjects |
title_full | Pharmacokinetics and safety of Enasidenib following single oral doses in Japanese and Caucasian subjects |
title_fullStr | Pharmacokinetics and safety of Enasidenib following single oral doses in Japanese and Caucasian subjects |
title_full_unstemmed | Pharmacokinetics and safety of Enasidenib following single oral doses in Japanese and Caucasian subjects |
title_short | Pharmacokinetics and safety of Enasidenib following single oral doses in Japanese and Caucasian subjects |
title_sort | pharmacokinetics and safety of enasidenib following single oral doses in japanese and caucasian subjects |
topic | Original Articles |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6199364/ https://www.ncbi.nlm.nih.gov/pubmed/30386625 http://dx.doi.org/10.1002/prp2.436 |
work_keys_str_mv | AT liyan pharmacokineticsandsafetyofenasidenibfollowingsingleoraldosesinjapaneseandcaucasiansubjects AT liuliangang pharmacokineticsandsafetyofenasidenibfollowingsingleoraldosesinjapaneseandcaucasiansubjects AT gomezdiana pharmacokineticsandsafetyofenasidenibfollowingsingleoraldosesinjapaneseandcaucasiansubjects AT chenjian pharmacokineticsandsafetyofenasidenibfollowingsingleoraldosesinjapaneseandcaucasiansubjects AT tongzeen pharmacokineticsandsafetyofenasidenibfollowingsingleoraldosesinjapaneseandcaucasiansubjects AT palmisanomaria pharmacokineticsandsafetyofenasidenibfollowingsingleoraldosesinjapaneseandcaucasiansubjects AT zhousimon pharmacokineticsandsafetyofenasidenibfollowingsingleoraldosesinjapaneseandcaucasiansubjects |