Gemigliptin is a prolyl-specific dipeptidyl aminopeptidase IV
(DPP IV, DPP-4, CD26) inhibitor approved for the treatment of type
2 diabetes mellitus by the Korean Food and Drug Administration in
2012. Gemigliptin was discovered and developed by LG Life
Sciences and is now the sixth DPP-4 inhibitor approved for the
treatment of type 2 diabetes. At the time this review was prepared,
there were no publications describing the discovery strategy
and preclinical data that led to the advancement of gemigliptin to the clinic.