Pharmacokinetics and pharmacodynamics of single-dose oral tolvaptan in fasted and non-fasted states in healthy Caucasian and Japanese male subjects.

European Journal of Clinical Pharmacology
Susan E ShoafSuresh Mallikaarjun

Abstract

To compare the pharmacokinetics and pharmacodynamics of tolvaptan in Caucasian and Japanese healthy male subjects under fasting and non-fasting conditions. This was a single-center, parallel-group, randomized, open-label, three-period crossover trial of single oral doses of tolvaptan 30 mg under fasting and non-fasting [a high-fat, high-calorie meal (HFM) or Japanese standard meal] conditions in 25 healthy male Caucasian subjects and 24 healthy male Japanese subjects. Pharmacodynamic endpoints were urine volume and fluid balance for 0 to 24 h postdose. In the fasted state, the plasma tolvaptan C(max) and AUC(∞) geometric mean ratios (90 % confidence interval) were 1.105 (0.845-1.444) and 1.145 (0.843-1.554) for Japanese compared to Caucasian subjects. A HFM increased the C(max) and AUC(∞) values by about 1.15-fold in both Japanese and Caucasian subjects.. Twenty-four-hour urine volumes paralleled pharmacokinetic changes, but the increases were not clinically significant. Fluid balance in the Japanese men was 1.4- to 2.0-fold more negative than that in the Caucasian men. Tolvaptan pharmacokinetics is not clinically significantly affected by race. Body weight is a factor that affects exposure. Tolvaptan can be administered with o...Continue Reading

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Citations

Jan 1, 2014·Journal of Clinical Medicine·Purav R BhattJ Herbert Patterson
Dec 15, 2015·Toxicological Sciences : an Official Journal of the Society of Toxicology·Jia-Long FangFrederick A Beland
Apr 8, 2014·Pharmacotherapy·Brian P Baur, Calvin J Meaney
Sep 27, 2015·Drugs·Hannah A Blair, Gillian M Keating
Apr 11, 2015·Biochemical Pharmacology·Yuanfeng WuJia-Long Fang
Oct 30, 2018·International Heart Journal·Koichiro KinugawaTakayuki Inomata
Aug 15, 2021·Molecular and Cellular Endocrinology·Giada MarronciniAlessandro Peri

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