Drug Res (Stuttg) 2016; 66(02): 74-81
DOI: 10.1055/s-0035-1549967
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

A Pharmacokinetic/Pharmacodynamic Drug–Drug Interaction Study of Tofogliflozin (a New SGLT2 Inhibitor) and Selected Anti-Type 2 Diabetes Mellitus Drugs

N. Kasahara
1   Clinical Research Planning Department, Chugai Pharmaceutical Co., Ltd., Tokyo, Japan
H. Fukase
2   CPC Clinical Trial Hospital, Medipolis Medical Research Institute, Kagoshima, Japan
Y. Ohba
1   Clinical Research Planning Department, Chugai Pharmaceutical Co., Ltd., Tokyo, Japan
T. Saito
1   Clinical Research Planning Department, Chugai Pharmaceutical Co., Ltd., Tokyo, Japan
K. Miyata
1   Clinical Research Planning Department, Chugai Pharmaceutical Co., Ltd., Tokyo, Japan
S. Iida
1   Clinical Research Planning Department, Chugai Pharmaceutical Co., Ltd., Tokyo, Japan
Y. Takano
1   Clinical Research Planning Department, Chugai Pharmaceutical Co., Ltd., Tokyo, Japan
S. Ikeda
1   Clinical Research Planning Department, Chugai Pharmaceutical Co., Ltd., Tokyo, Japan
M. Harigai
3   Department of Pharmacovigilance, Graduate School of Medical and Dental Sciences, Tokyo Medical and Dental University, Tokyo, Japan
K. Terao
1   Clinical Research Planning Department, Chugai Pharmaceutical Co., Ltd., Tokyo, Japan
› Author Affiliations
Further Information

Publication History

received 23 January 2015

accepted 21 April 2015

Publication Date:
09 July 2015 (online)


Objective: Tofogliflozin is an oral hypoglycemic agent with a novel mechanism of action that reduces blood glucose levels by promoting glucose excretion in urine, achieved by selectively inhibiting sodium-glucose co-transporter 2 (SGLT2). We evaluated the effects of several selected anti-type 2 diabetes mellitus (T2DM) drugs-glimepiride, metformin, sitagliptin, pioglitazone, miglitol, nateglinide, and voglibose-on the pharmacokinetics and pharmacodynamics of tofogliflozin, and the effects of tofogliflozin on the pharmacokinetics of these anti-T2DM drugs in healthy male volunteers.

Methods: A single dose of either tofogliflozin alone, one of the anti-T2DM drugs alone, or co-administration of tofogliflozin and the anti-T2DM drug was administered to 108 healthy men. Cmax, AUCinf, and cumulative urine glucose excretion after co-administration of tofogliflozin and each of the anti-T2DM drugs was evaluated relative to the values of those parameters after administration of each drug alone.

Results: None of the anti-T2DM drugs had any effect on tofogliflozin exposure. Tofogliflozin had no or little effect on the exposure of any anti-T2DM drug. No anti-T2DM drug had any major effect on the cumulative urine glucose excretion induced by tofogliflozin. There were no safety concerns evident after administration of any drug alone or in co-administration.

Conclusions: Neither the pharmacokinetics nor the pharmacodynamics of tofogliflozin was affected by any of the anti-T2DM drugs evaluated in this study, nor was the pharmacokinetics of any of the anti-T2DM drugs affected by tofogliflozin in healthy male volunteers.

Supporting Information

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