Dipeptidyl Peptidase-4 Inhibitor
Introduction
Inhibitors of dipeptidyl peptidase 4 (DPP-4
inhibitors or gliptins) are a class of drug that act as oral
hypoglycemics that block the enzyme dipeptidyl
peptidase-4 (DPP-4).
 They can be used to treat diabetes mellitus type 2
Commonly known as Gliptins
Who are Gliptins?
Sitagliptin (FDA approved 2006, marketed by Merck &
Co. as Januvia)
Vildagliptin (EU approved 2007, marketed in the EU
by Novartis as Galvus)
Saxagliptin (FDA approved in 2009, marketed as Onglyza)
How Gliptins Works
Pharmacokinetics of Gliptins
well absorbed after oral administration.
Food does not affect the extent of absorption.
Alogliptin and sitagliptin are mostly excreted
unchanged in the urine.
Saxagliptin is metabolized via CYP450 3A4/5 to an
active metabolite.
The primary route of elimination for saxagliptin and
the metabolite is renal.
All DPP-4 inhibitors except linagliptin require dosage
adjustments in renal dysfunction
Adverse effects gliptins
Nasopharyngitis
Headache
Nausea
 Heart failure ,
Hypersensitivity and
Skin reactions