This randomized, placebo-controlled within dose groups, double-blind, single 
rising dose study investigated the safety, tolerability, pharmacokinetics and 
pharmacodynamics of 1 mg to 100 mg doses of empagliflozin in 48 healthy Japanese 
male subjects. Empagliflozin was rapidly absorbed, reaching peak levels in 1.25 
to 2.50 h; thereafter, plasma concentrations declined in a biphasic fashion, 
with mean terminal elimination half-life ranging from 7.76 to 11.7 h. Increase 
in empagliflozin exposure was proportional to dose. Oral clearance was dose 
independent and ranged from 140 to 172 mL/min. In the 24 h following 100 mg 
empagliflozin administration, the mean (%CV) amount of glucose excreted in urine 
was 74.3 (17.1) g. The amount and the maximum rate of glucose excreted via urine 
increased with dose of empagliflozin. Nine adverse events, all of mild 
intensity, were reported by 8 subjects (7 with empagliflozin and 1 with the 
placebo). No hypoglycemia was reported. In conclusion, 1 mg to 100 mg doses of 
empagliflozin had a good safety and tolerability profile in healthy Japanese 
male subjects. Exposure to empagliflozin was dose proportional. The amount and 
rate of urinary glucose excretion were higher with empagliflozin than with the 
placebo, and increased with empagliflozin dose.