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. 2008 Oct;1(8):39–48.

Table 7.

In the Pipeline: Selected Emerging Antihyperglycemic Compounds

Drug category Mechanism of action Comments
Glucokinase activators Activate key enzymes to increase hepatic glucose metabolism Several drugs are currently in phase 2 clinical trials
Sodium-glucose cotransporter 2 inhibitors Inhibit reabsorption of glucose at the proximal tubule of the kidney, thereby decreasing systemic hyperglycemia Low potential for hypoglycemia
11β-hydroxysteroid dehydrogenase 1 (11β-HSD 1) inhibitors Inhibit an enzyme responsible for activating cortisone to cortisol, thus minimizing antiglycemic effects of cortisol Low potential for hypoglycemia, may have beneficial effects on metabolic syndrome
Glucagon receptor antagonists Block glucagon from binding to hepatic receptors, thereby decreasing gluconeogenesis Low potential for hypoglycemia
Cannabinoid-1 (CB-1) receptor antagonists Block CB-1 receptors systemically Marketed as an obesity drug, may cause psychiatric symptoms

Source: Inzucchi SE, McGuire DK. New drugs for the treatment of diabetes mellitus: part II: incretin-based therapy and beyond. Circulation. 2008;117:574–584.