The Place of Dipeptidyl Peptidase-4 Inhibitors in Type 2 Diabetes Therapeutics: A “Me Too” or “the Special One” Antidiabetic Class?
Table 3
Main characteristics of the DPP-4 inhibitors already approved for use in the US and/or EU market: sitagliptin, vildagliptin, saxagliptin, alogliptin, and linagliptin.
Sitagliptin
Vildagliptin
Saxagliptin
Alogliptin
Linagliptin
Dosing
100 mg qd
50 mg bid
5 mg qd
25 mg qd
5 mg qd
Max. DPP-4 inhibition (%)
±97
±95
70–80
>90
>90
Selectivity for DPP-4
High
High
Moderate
High
High
HbA1c reduction (%)
0.5–1.0
0.9 (mean value)
0.5–1.0
0.6 (mean value)
0.5–0.7
Hypoglycaemic risk
Low
Low
Low
Low
Low
Half-life compound (, h)
±12
1.5–3
±2.5
11–22
>100
Bioavailability (%)
±87
±85
±67
—
±30
Metabolism/ elimination
Renal excretion almost unchanged (70–80% parent)
Renal excretion (±26% parent and ±55% as metabolite obtained after hydrolysis)
Liver metabolized to active metabolite by P450 3A4/5 and renal excretion (12–29% unchanged parent and 21–52% as metabolite)
Renal excretion almost unchanged parent (60–70%)
Biliary excretion almost unchanged (>70% unchanged parent) and renal (<6%)
Adapted from [93–99] using available information/knowledge. HbA1c variations vary between studies and depend on baseline levels. Values presented are the range or mean value calculated from the studies available.
