Type 2 diabetes mellitus is a chronic disease most often characterized by increased glucose levels. When blood glucose levels are inadequately controlled or left untreated, the result is a variety of microvascular and macrovascular complications. To prevent these outcomes, many medications are available to manage type 2 diabetes mellitus and prevent disease progression. However, most of the medications available to date only target a few of the physiological defects caused by diabetes and may come with side effects that make adherence to the medication improbable. Imeglimin, a medication currently under investigation in the United States and approved in Japan, is a novel, first-in-its-class medication with a mechanism that is currently understood to target multiple pathways to provide glycemic control. This review aims to present and discuss the current clinical and scientific evidence pertaining to imeglimin.