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.