Dorzagliatin regulates glucose-stimulated GLP-1 release and improves glycemic control with good tolerance when combined with sitagliptin in patients with T2D and obesity, suggesting the role of dorzagliatin in the regulation of GLP-1 release in response to oral glucose challenge in a triple acting role of regulation of glucose homeostasis. Here, GCG is linked to obesity due to melanocortin 4 receptor deficiency.