Pharmacology · Class
DPP-4 inhibitors (gliptins) !
Oral drugs that stop the breakdown of the body's own gut hormones (incretins), so insulin rises after meals. Gentle and weight-neutral.
Updated 2026-11-01
What they are
Inhibitors of the enzyme dipeptidyl peptidase-4. Used in type 2 diabetes, usually added to metformin.
Mechanism of action
DPP-4 is a serine protease on cell surfaces and in plasma that inactivates GLP-1 and GIP within minutes by cutting two amino acids off their N-terminus. Gliptins block it, so active incretin levels rise after meals; insulin release increases and glucagon falls, both in a glucose-dependent way.
Target: Dipeptidyl peptidase-4 (DPP4, CD26)
Drugs in this class
- SitagliptinThe first DPP-4 inhibitor: an oral tablet that protects the body's own incretins, with low hypoglycemia risk and no…Dipeptidyl peptidase-4 (DPP-4)
- LinagliptinA DPP-4 inhibitor cleared mainly through bile, so it needs no kidney adjustment. Low hypoglycemia risk, no weight…Dipeptidyl peptidase-4 (DPP-4)
- SaxagliptinA DPP-4 inhibitor metabolized by CYP3A4. It raised heart failure hospitalizations in a large trial, so it is avoided…Dipeptidyl peptidase-4 (DPP-4)
- VildagliptinA DPP-4 inhibitor used in Europe and other regions, not in the US. It binds the enzyme covalently and is cleared…Dipeptidyl peptidase-4 (DPP-4)
Others in the class
- alogliptin
Test yourself
Think of the answer, then tap the question to see it.
Which hormones does DPP-4 inactivate?
The incretins GLP-1 and GIP, by removing the first two amino acids from their N-terminal end.
Which gliptin needs no kidney adjustment, and why?
Linagliptin, because it is eliminated mainly unchanged through bile and feces rather than urine.
Why are DPP-4 inhibitors weight-neutral while GLP-1 agonists cause weight loss?
They only raise the body's own incretins to physiological levels, too low to slow the stomach or reduce appetite much.
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Sitagliptin: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); DailyMed - SITAGLIPTIN tablet, film coated (DailyMed (U.S. National Library of Medicine), 2026); HUMAN DIPEPTIDYL PEPTIDASE IV IN COMPLEX WITH A BETA AMINO ACID INHIBITOR (RCSB Protein Data Bank, 2005).
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Representative model, for educational purposes only.