Dataset Information

Pharmacokinetics and Pharmacodynamics of Ertugliflozin in Healthy Japanese and Western Subjects.

ABSTRACT: Ertugliflozin, a sodium-glucose cotransporter 2 inhibitor, is approved for treatment of type 2 diabetes. This randomized, double-blind (sponsor-open) study in healthy Japanese subjects and open-label study in Western subjects assessed ertugliflozin pharmacokinetics and pharmacodynamics. Cohort A received 3 ascending single doses of ertugliflozin (1, 5, and 25 mg; n = 6 Japanese, n = 6 Western) or placebo (n = 3 Japanese) under fasted conditions. Cohort B received multiple once-daily doses of ertugliflozin 25 mg (n = 6 Japanese) or placebo (n = 3 Japanese) for 7 days under fed conditions. For Japanese subjects in Cohort A, maximum plasma concentrations (C_max ) were observed 1 to 1.5 hours after dosing, and apparent mean terminal half-life was 12.4 to 13.6 hours. The ratios of the geometric means (Japanese/Western) for ertugliflozin 1-, 5-, and 25-mg single doses were 95.94%, 99.66%, and 90.32%, respectively, for area under the plasma concentration-time curve and 107.59%, 97.47%, and 80.04%, respectively, for C_max . Area under the plasma concentration-time curve and C_max increased in a dose-proportional manner. For Cohort B, C_max was observed 2.5 hours after dosing (days 1 and 7), and steady state was reached by day 4. The 24-hour urinary glucose excretion was dose dependent. Ertugliflozin was generally well tolerated. There were no meaningful differences in exposure, urinary glucose excretion, and safety between Japanese and Western subjects.

SUBMITTER: Li Y

PROVIDER: S-EPMC8359436 | biostudies-literature | 2021 Jul

REPOSITORIES: biostudies-literature

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Pharmacokinetics and Pharmacodynamics of Ertugliflozin in Healthy Japanese and Western Subjects.

Li Yinhua Y Nucci Gianluca G Yamamoto Yuichi Y Fediuk Daryl J DJ Sahasrabudhe Vaishali V

Clinical pharmacology in drug development 20210112 7

Ertugliflozin, a sodium-glucose cotransporter 2 inhibitor, is approved for treatment of type 2 diabetes. This randomized, double-blind (sponsor-open) study in healthy Japanese subjects and open-label study in Western subjects assessed ertugliflozin pharmacokinetics and pharmacodynamics. Cohort A received 3 ascending single doses of ertugliflozin (1, 5, and 25 mg; n = 6 Japanese, n = 6 Western) or placebo (n = 3 Japanese) under fasted conditions. Cohort B received multiple once-daily doses of ert ...[more]

PMID: 33434408

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Dataset Information

Pharmacokinetics and Pharmacodynamics of Ertugliflozin in Healthy Japanese and Western Subjects.

Publications

Pharmacokinetics and Pharmacodynamics of Ertugliflozin in Healthy Japanese and Western Subjects.

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