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Following in vitro tests, compound 57 (Figure 7) was shown to be the most potent DPP-4 inhibitor, with an IC 50 of 0.87 nM

-cell-selective knockout of the GLP-1R in mice with impaired glucose tolerance after intraperitoneal injection of glucose and exogenous supplementation of GLP-1 did not induce insulin secretion, but glucose tolerance returned to normal after oral glucose, suggesting that the extra-islet GLP-1R plays a regulatory role in oral glucose tolerance (Smith et al., 2014)

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BDNF levels and genotype are associated with antipsychotic-induced weight gain in patients with chronic schizophrenia

Competition between major pharmaceutical companies is accelerating innovation in oral GLP-1 therapies, especially in small-molecule drug development

The once-daily subcutaneously administered GLP-1RA liraglutide (Victoza) was approved for the treatment of type 2 diabetes (in doses up to 1.8 mg) by the European Medicines Agency in 2009 and by the US Food and Drug Administration in 2010