ATC Code A10BH01
Formula C16H15F6N5O
Molar Mass (g·mol−1) 407,31
Physical State solid
PKS Value 8.78
CAS Number 486460-32-6
PUB Number 4369359
Drugbank ID DB01261
Solubility soluble in water


Sitagliptin is an oral antidiabetic medication used to treat type 2 diabetes. Sitagliptin is an oral dipeptidyl peptidase-4 (DPP-4) inhibitor used in conjunction with diet and exercise to improve blood sugar control. It is taken by mouth. It is also available in the fixed-dose combination medication sitagliptin/metformin.



Inhibition of DPP-4 by sitagliptin slows DPP-4-mediated inactivation of incretins such as GLP-1 and GIP. Incretins are released throughout the day and upregulated in response to meals as part of glucose homeostasis. Decreased inhibition of incretins increases insulin synthesis and decreases glucagon release in a glucose concentration-dependent manner. These effects result in an overall improvement in glycemic control, as evidenced by reduced glycosylated hemoglobin (HbA1c).


Sitagliptin is 87% orally bioavailable and taking it with or without food does not affect its pharmacokinetics. Sitagliptin reaches maximum plasma concentration within 2 hours. Protein binding is approximately 38%. Sitagliptin is largely unmetabolized, with 79% of the dose excreted in the urine as the unchanged parent compound. Minor metabolic pathways are mediated primarily by cytochrome p450 CYP3A4 and to a lesser extent by CYP2C8. The plasma half-life is approximately 12.4 hours.


Side effects

Common side effects are headache, swelling of the legs, and upper respiratory tract infection. Serious side effects may include angioedema, low blood sugar, kidney problems, pancreatitis, and joint pain. It is unclear whether it is safe to use during pregnancy or breastfeeding.


  • PubChem
  • Drugbank
  • Aktories, Förstermann, Hofmann, Starke: Allgemeine und spezielle Pharmakologie und Toxikologie, Elsvier, 2017

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Markus Falkenstätter

Markus Falkenstätter

Markus Falkenstätter is a writer on pharmaceutical topics in Medikamio's medical editorial team. He is in the last semester of his pharmacy studies at the University of Vienna and loves scientific work in the field of natural sciences.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer

Stefanie Lehenauer has been a freelance writer for Medikamio since 2020 and studied pharmacy at the University of Vienna. She works as a pharmacist in Vienna and her passion is herbal medicines and their effects.

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