INS and Insulin resistance: In this study, we discuss the glucose-lowering mechanisms of imeglimin, the ability to decrease HbA1c via imeglimin treatment in clinical trials, the effects of imeglimin on the markers of insulin secretion and insulin resistance and on serum lipids, the safety profile of imeglimin, the effects of imeglimin on endothelial dysfunction, the beneficial effects of imeglimin on the diabetic complications observed in animals, concepts that are currently being demonstrated, and matters requiring elucidated in the future with regard to the abovementioned issues.