Journal of Diabetes Research / 2015 / Article / Tab 3

Review Article

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.

SitagliptinVildagliptinSaxagliptinAlogliptin Linagliptin

Dosing 100 mg qd50 mg bid5 mg qd25 mg qd5 mg qd

Max. DPP-4 inhibition (%)±97±9570–80>90>90

Selectivity for DPP-4HighHighModerateHighHigh

HbA1c reduction (%)0.5–1.00.9 (mean value)0.5–1.00.6 (mean value)0.5–0.7

Hypoglycaemic riskLowLowLowLowLow

Half-life compound (, h)±121.5–3±2.511–22>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 [9399] 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.

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