Diabetes is one of the major diseases worldwide and is the third leading cause of death in the United States. Anti-diabetic drugs are used in the treatment of diabetes mellitus to control glucose levels in the blood. Most of the drugs are administered orally, except for a few of them, such as insulin, exenatide, and pramlintide. In this review, we are going to discuss seven major types of anti-diabetic drugs: Peroxisome proliferator-activated receptor (PPAR) agonist, protein tyrosine phosphatase 1B (PTP1B) inhibitors, aldose reductase inhibitors, α-glucosidase inhibitors, dipeptidyl peptidase IV (DPP-4) inhibitors, G protein-coupled receptor (GPCR) agonists and sodium-glucose co-transporter (SGLT) inhibitors. Here, we are also discussing some of the recently reported anti-diabetic agents with its multi-target pharmacological actions. This review summarises recent approaches and advancement in anti-diabetes treatment concerning characteristics, structure-activity relationships, functional mechanisms, expression regulation, and applications in medicine.
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