Chemical structure:

IUPAC name:

(R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine

CAS number:

486460-32-6

Therapy area:

Anti-diabetic

References:

IH

Status:

Commercial scale

Mechanism of action

The dipeptidyl peptidase 4 (DPP-4) enzyme is competitively inhibited by sitagliptin (DPP-4). The digestive hormones GLP-1 and GIP, which are secreted in response to food, are broken down by this enzyme.  They are able to boost the production of insulin and decrease the release of glucagon by the pancreatic alpha cells by blocking the breakdown of GLP-1 and GIP. [Required medical citation] Blood glucose levels go closer to normal as a result. [Required medical citation] The quantities of insulin produced and glucagon inhibited decrease as blood glucose levels go closer to normal, helping to prevent a “overshoot” and consequent low blood sugar.

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