Enzymes

DPP-4

Dipeptidyl peptidase 4

Also known as: DPP-4, CD26, dipeptidyl-peptidase-4

What it is

Membrane enzyme (CD26) that degrades incretin peptides (GLP-1 and GIP), reducing glucose-stimulated insulin secretion. It is the therapeutic target of gliptins (sitagliptine, vildagliptine, saxagliptine).

Role in interactions

DPP-4 inhibitors (gliptins) prolong incretin action and increase insulin secretion; should not be combined with insulin or secretagogues without dose adjustment (hypoglycaemia risk).

Common substrates

Substrates: GLP-1, GIP (endogenous incretin peptides).

Inhibitors

Inhibitors: sitagliptine, vildagliptine, saxagliptine, linagliptine.

Inducers

Inducers: there are no clinically relevant inducers.

Clinical notes

Gliptins are well tolerated; caution in renal impairment (dose adjustment for sitagliptine, saxagliptine, vildagliptine); linagliptine does not require renal adjustment.

Source

DailyMed/FDA (NIH/NLM) — approved labels (sitagliptine, vildagliptine, saxagliptine); EMC-UK (MHRA) — SmPC