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Pharmacol Res Perspect. 2018 Oct 23;6(6):e00436. doi: 10.1002/prp2.436. eCollection 2018 Dec.

Pharmacokinetics and safety of Enasidenib following single oral doses in Japanese and Caucasian subjects.

Author information

1
Translational Development and Clinical Pharmacology Celgene Corporation Summit New Jersey.
2
Biostatistics Celgene Corporation Summit New Jersey.
3
Non-Clinical Development Celgene Corporation Summit New Jersey.

Abstract

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.

KEYWORDS:

Caucasian; Enasidenib; IDHIFA; Japanese; pharmacokinetics; race

PMID:
30386625
PMCID:
PMC6199364
DOI:
10.1002/prp2.436
[Indexed for MEDLINE]
Free PMC Article

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