Dipeptidyl Peptidase-4 Inhibitors (DPP-4 Inhibitors, Gliptins)

Agents

Alogliptin: FDA approved in 2013
Anagliptin: approved in Japan in 2012
Berberine: herbal dietary supplement which inhibits dipeptidyl peptidase-4 (which at least partly explains its antihyperglycemic activity)
Dutogliptin: in development
Gemigliptin: in development
Linagliptin (Tradjenta): FDA approved in 2011
Lupeol: present in mango, red alder (Alnus rubra), and dandelion coffee
Omarigliptin (MK-3102): in development
Saxagliptin (Onglyza): FDA approved in 2009
Sitagliptin (Januvia) (see Sitagliptin, [[Sitagliptin]]): FDA approved 2006
Teneligliptin: approved in Japan in 2012
Trelagliptin: approved in Japan in 2015
Vildagliptin (Galvus): approved in EU in 2007

Epidemiology: possibly increased risk of angioedema when used in combination with angiotensin converting enzyme (ACE) inhibitors (see Angiotensin Converting Enzyme Inhibitors, [[Angiotensin Converting Enzyme Inhibitors]])
Pharmacology
- DPP-4 plays a significant role in the degradation of bradykinin once ACE activity is reduced
- DPP-4 primarily degrades substance P at its amino terminus when ACE is inhibited -> this kinin likely facilitates the occurrence of angioedema by the activation of neurokinin receptor 1

Angioedema induced by cardiovascular drugs: new players join old friends. Allergy. 2015 Oct;70(10):1196-200. doi: 10.1111/all.12680. Epub 2015 Jul 15 [MEDLINE]