Imeglimin is an investigational first‐in‐class novel oral agent for the treatment of type 2 diabetes Mellitus (T2DM). Several pivotal phase III trials have been completed with evidence of significant glucose lowering and a generally favourable safety and tolerability profile, including the lack of severe hypoglycaemia.

Imeglimin's mechanism of action involves dual effects: (a) amplification of glucose‐stimulated insulin secretion (GSIS) and preservation of β‐cell mass; and (b) enhanced insulin action, including the potential for inhibition of hepatic glucose output and improvement in insulin signalling in both liver and skeletal muscle.

At a cellular and molecular level, Imeglimin's underlying mechanism may involve correction of mitochondrial dysfunction, a common underlying element of T2D pathogenesis. It has been observed to rebalance respiratory chain activity (partial inhibition of Complex I and correction of deficient Complex III activity), resulting in reduced reactive oxygen species formation (decreasing oxidative stress) and prevention of mitochondrial permeability transition pore opening (implicated in preventing cell death).