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01.04.2015 | Original Research | Ausgabe 4/2015 Open Access

Advances in Therapy 4/2015

Pharmacokinetics, Pharmacodynamics, and Safety of Luseogliflozin in Japanese Patients with Type 2 Diabetes Mellitus: A Randomized, Single-blind, Placebo-controlled Trial

Advances in Therapy > Ausgabe 4/2015
Takashi Sasaki, Yutaka Seino, Atsushi Fukatsu, Michito Ubukata, Soichi Sakai, Yoshishige Samukawa
Wichtige Hinweise

Electronic supplementary material

The online version of this article (doi:10.​1007/​s12325-015-0200-x) contains supplementary material, which is available to authorized users.
Trial registration: Japan Pharmaceutical Information Center; Identifier: JapicCTI-090909.



Luseogliflozin, a potent, selective sodium glucose cotransporter 2 inhibitor, promotes urinary glucose excretion (UGE) and reduces plasma glucose concentrations. Luseogliflozin was approved for use in Japan after favorable pharmacokinetic, pharmacodynamic, and safety profiles were reported in healthy Japanese subjects and patients with type 2 diabetes mellitus (T2DM) in clinical development studies. We aimed to investigate the pharmacokinetics, pharmacodynamics, and safety of multiple doses of luseogliflozin administered once daily for 7 days in Japanese patients with T2DM.


We conducted a randomized, placebo-controlled, single-blind, parallel-group, clinical pharmacology study at the P-One Clinic, Keikokai Medical Corporation (Tokyo, Japan) between August 2009 and November 2009. Forty Japanese patients with T2DM were randomly assigned to receive once-daily 0.5, 1, 2.5 or 5 mg luseogliflozin or placebo for 7 days. We assessed the pharmacokinetics, pharmacodynamics (including changes in UGE and plasma glucose concentrations), and safety of luseogliflozin.


The plasma concentrations of luseogliflozin and its active metabolite, M2, were dose proportional, without accumulation. 24-h UGE was greater in all luseogliflozin groups versus placebo. Least-squares mean differences in 24-h UGE on Day 7 increased dose dependently in the luseogliflozin groups, with values of 49.2, 66.5, 89.4, and 101 g/day at 0.5, 1, 2.5, and 5 mg, respectively. On Day 7, the areas under the concentration–time curves for post-meal plasma glucose and the mean plasma glucose for 0–16 h were significantly lower in all luseogliflozin groups versus placebo. Seven patients had mild adverse events (AEs); all were resolved. No AEs led to study discontinuation.


Once-daily administration of luseogliflozin for 7 days increased 24-h UGE in a dose-dependent manner, reduced plasma glucose concentrations, and was well tolerated in Japanese patients with T2DM. The pharmacokinetic and pharmacodynamic profile of luseogliflozin observed in this study supports its once-daily dosing regimen.


Taisho Pharmaceutical Co., Ltd.

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