Single Ascending-Dose Studies (SADs)

Each cohort consisted of six randomized subjects receiving imeglimin and two or three receiving a placebo. Imeglimin or placebo was administered to Caucasian and Japanese subjects in single oral doses of 250 (Caucasian only), 500, 1000, 1500, 2000, 4000, 6000, and 8000 (Caucasian only) mg on the morning of Day 1 after an overnight fasting period. Blood samples (6 mL) for plasma pharmacokinetic assessments were collected into a lithium heparinate tube on Day 1 at the following time points: pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48, and 72 h post-dose, except for Caucasians at 1000, 1500, 2000, and 4000 mg where the following timepoints were used: pre-dose, 1, 2, 3, 3.5, 4, 4.5, 5, 6, 8, 12, 16, 24, 36, 48, and 72 h post-dose. Urine samples were collected for each cohort: before drug administration, and at the following intervals 0–4, 4–8, 8–12, 12–24, and 24–48 h after drug administration.