Background: Irsogladin maleate, increasing gastric mucosal blood flow and cAMP in mucosal epithelial cells, is being marketed for the treatment of gastric ulcer and gastritis. The object of this study was to evaluate the pharmacokinetic characteristics and safety profiles of irsogladin maleate in Koreans. Methods: An open-label, dose-escalation, parallel group study was conducted in 28 healthy male Korean volunteers. Irsogladin maleate was administered as a single dose of 4 mg (n=16), 8 mg (n=6) or 16 mg (n=6). Serial blood samples for pharmacokinetic analysis were taken over 504 h. Plasma concentration of irsogladin was measured by high performance liquid chromatography-tandem mass spectrometry (LC-MS/MS). Pharmacokinetic parameters were determined using noncompartmental methods. Laboratory tests, ECGs, vital signs and physical examinations were performed for clinical safety evaluation. Results: Maximum observed irsogladin plasma concentration ($C_{max}$) (mean $pm$ SD) of 4 mg, 8 mg and 16 mg dosage group were $82.9;{pm};12.5{mu};g/L$, $161.4;{pm};25.9;{mu}g/L$ and $292.6;{pm};51.2;{mu}g/L$, respectively. Area under the plasma concentration versus time curve from dosing to the last quantifiable concentration ($AUC_{last}$) of three dosage groups were $12694.4;{pm}2906.2;{mu}g;{ast}h/L$, $24970.0;{pm};5253.8;{mu}g;{ask}h/L$,$47125.3;{pm};8676.7;{mu}g;{ast}h/L$, respectively. Apparent clearance ($0.30;{pm};0.07L/H$, $0.31;{pm};0.10;L/H$, $0.31;{pm};0.06;L/H$, respectively) was unaffected by dosage. The 95% CI of slope of Dose-$C_max$ and Dose-$AUC_{last}$ linear regression were 15.4-19.6 and 2485.2-3262.0. All adverse events reported were mild and no clinically significant abnormalities of safety evaluation were observed. Conclusions: The pharmacokinetic characteristics of Irsogladin maleate after single dose dministration was explored in healthy Korean volunteers. Irsogladin maleate displayed linear plasma pharmacokinetics over the dose range 4-16 mg. Irsogladin maleate was well tolerated after single dose administration in Koreans.