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


  • 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

Adverse Effects

Allergic/Immunologic Adverse Effects

Angioedema (see Angioedema, [[Angioedema]])

  • 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

Other Averse Effects

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  • 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]