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. 2022 May 10;27(10):3055. doi: 10.3390/molecules27103055

Table 1.

The features of approved dipeptidyl peptidase 4 inhibitors (DPP4i).

DPP4i Chemistry Metabolism Half-Life Elimination Method
Sitagliptin β-amino acid based Minimal 12.5 h Predominantly
(>80%) renal
Vildagliptin Cyanopyrrolidine Hydrolysis
(cytochromeindependent)
to form an inactive
metabolite
~2 h Metabolism
(parent)
and renal
(metabolite)
Saxagliptin Cyanopyrrolidine Hydrolysis (cytochrome P450 3A4
or P450 3A5) to form an activemetabolite
2.5 h (parent),
3 h (metabolite)
Metabolism
(parent)
and renal
(metabolite)
Alogliptin Modified
pyrimidinedione
Minimal 20 h Predominantly
(>70%)
renal
Linagliptin Xanthine
based
Minimal ~12 h (effective),
>100 h (terminal)
Predominantly
biliary
(<6% renal)