Background: Bepotastine besilate is a non-sedating, second-generation $H_1$-antagonist. It is known to be rapidly absorbed after oral administration and negligibly distributed to the brain. This study aimed to assess pharmacokinetic (PK) characteristics and safety of bepotastine besilate after oral administration in Korean healthy subjects. Methods: An open, single dose, parallel group, dose-escalation study was performed in sixteen healthy subjects. Two groups of eight subjects received either 10 or 20 mg dosage, respectively. Blood samples for PK assessments were collected till 24 hours after oral administration of bepotastine besilate. For safety assessments, clinical laboratory tests, vital signs, physical examinations, and 12-lead ECGs(electrocardiographies) were measured. Results: The average area under the concentration-time curves from time zero to infinity (AUC) were $397.12{pm}28.56;(Mean{pm}SD);{mu}g{cdot}h/L$ for the 10 mg group, and $776.80{pm}88.48;{mu}g{cdot}h/L$ for the 20 mg group. The values of average $C_{max}$ were $97.19{pm}22.72;{mu}g/L$ and $188.79{pm}30.39;{mu}g/L$ in the 10 mg and 20 mg group, respectively. AUC and $C_{max}$ appeared to increase proportionally with the dose, and dose-normalized AUC and $C_{max}$ were similar between 10 mg and 20 mg dosing groups (t-test, P=0.647 647 and 0.777, respectively). Only one adverse event (hordeolum) was reported during this trial. No clinically significant abnormalities were observed in laboratory tests, vital signs or ECG measurements. Conclusions: Bepotastine besilate $C_{max}$ and AUC values proportionally increased with increasing dose. Bepotastine besilate was generally safe and well tolerated with only a mild adverse event.