Pharmacokinetics of T-614 after Single Oral Administration in Healthy Korean Volunteers

건강한 한국인 자원자에서 T-614의 단회 경구 투여 후 약동학적 특성에 대한 연구

Background: Iguratimod is a new type of disease modifying anti-rheumatic drug, which reduced the production of inflammatory cytokines. The purpose of this study was to evaluate pharmacokinetic characteristics and safety profiles of iguratimod after a single oral administration in healthy Korean volunteers. Methods: A randomized, double-blind, placebo-controlled, parallel group, single oral dose study was conducted in 24 healthy male volunteers. Three groups of eight subjects each received 25 mg, 50 mg, or 100 mg dosage, respectively. Two subjects in each dose group were administered matching placebo. Plasma concentrations of iguratimod were measured till 72 hours after drug administration. Tolerability was evaluated by monitoring adverse events, clinical laboratory tests, and 12-lead electrocardiograms. Results: The mean area under the concentration-time curve from 0 to 72 hours ($AUC_{last}$) were 11.9, 25.2, and 51.8 $mg{\times}h/L$ and the maximum plasma concentration ($C_{max}$) were 1.15, 2.33, and 4.78 mg/L in 25, 50 and 100 mg dose groups, respectively. All doses of iguratimod were well tolerated without serious adverse events or clinically meaningful changes. Conclusion: $C_{max}$ and $AUC_{last}$ values of iguratimod proportionally increased with incremental dose. Iguratimod was generally safe and well tolerated.