IntroductionLuseogliflozin, a sodium glucose cotransporter 2 inhibitor, inhibits reabsorption of glucose in the proximal renal tubule. It was developed for the treatment of type 2 diabetes mellitus.MethodsFor this first human study of luseogliflozin, randomized, single-blind, placebo-controlled, single ascending dose (1–25 mg) and multiple ascending dose (5 or 10 mg/day, 7 days) trials were conducted in healthy male Japanese subjects to investigate safety, pharmacokinetics, and pharmacodynamics.ResultsThere were no serious adverse events, adverse events leading to discontinuation, or episodes of hypoglycemia. After administration of a single oral dose of luseogliflozin, its maximum plasma level (C max) and area under the concentration–time curve increased in a dose-dependent manner, and no food effects were observed on pharmacokinetics. The mean time taken to reach C max (T max) ranged from 0.667 to 2.25 h. The mean plasma half-life of luseogliflozin (T 1/2) after multiple dosing for 7 days ranged from 9.14 to 10.7 h, and no detectable accumulation of luseogliflozin was observed. Urinary glucose excretion increased in a dose-dependent manner, ranging from 18.9 to 70.9 g (single-dose study).ConclusionLuseogliflozin was well tolerated and showed favorable pharmacokinetic and pharmacodynamic profiles in healthy male Japanese subjects.Electronic supplementary materialThe online version of this article (doi:10.1007/s12325-014-0102-3) contains supplementary material, which is available to authorized users.