J Korean Soc Clin Pharmacol Ther.  2013 Dec;21(2):150-158. 10.12793/jkscpt.2013.21.2.150.

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

• Shin D
• Kim BH
• Kim JR
• Lim KS
• Jang IJ
• Shin SG
• Yu KS

• KMID: 2203228
• DOI: http://doi.org/10.12793/jkscpt.2013.21.2.150

Abstract

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 (AUClast) were 11.9, 25.2, and 51.8 mg x h/L and the maximum plasma concentration (Cmax) 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
Cmax and AUClast values of iguratimod proportionally increased with incremental dose. Iguratimod was generally safe and well tolerated.

Keyword

Iguratimod; Pharmacokinetics; Korean

MeSH Terms

Administration, Oral*
Cytokines
Electrocardiography
Humans
Male
Pharmacokinetics*
Plasma
Cytokines

Figure

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  Figure 1. Mean plasma concentration-time profiles after oral administration of Iguratimod 25, 50 and 100 mg in healthy Korean subjects. Left panel, semi-log scale; right panel linear scale. Bars represent standard deviations.

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  Figure 2. Relationship between pharmacokinetic parameters and dose following single oral Iguratimod doses of 25, 50 and 100 mg. Left panel, log-transformed Cmax-dose relationship and right panel, log-transformed AUClast-dose relationship of Iguratimod.

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  Figure 3. Comparison of dose-normalized Cmax and AUClast after single oral administration of Iguratimod 25, 50 and 100 mg. The box edges show lower (25 th) and upper (75 th) quartiles and the line in the middle indicates the median value. Left panel, dose-normalized Cmax and right panel, dose-normalized AUClast.

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