Translations:Discovery and development of dipeptidyl peptidase-4 inhibitors/67/en
| Drug | Absorption | Bioavailability (%) | IC50 (nM) | Mean volume of distribution (L) | Protein binding (%) | Half-life (hours,100 mg dose) | Metabolism | Excretion |
|---|---|---|---|---|---|---|---|---|
| Sitagliptin | Rapidly absorbed with peak concentration at 1–4 hours | 87 | 18 | 198 | 38 | 12.4 | Small fraction undergoes hepatic metabolism via CYP 450 3A4 and 2C8 | Excreted in an unchanged form in the urine (79%) |
| Vildagliptin | Rapidly absorbed with peak concentration at 1–2 hours | 85 | 3 | 70.5 | 9.3 | 1.68 (once a day) and 2.54 (twice a day) | Hydrolysis resulting in a pharmacologically inactive metabolite. A fraction (22%) is also excreted unchanged by the kidneys | Excretion of the metabolite is carried out through urine (85%) and feces (15%) |