Comparison of DPP-4 inhibitors to be developed
| Enzyme Inhibition In Vivo after 24 h (ED50) | IC50 | DPP-4 Inhibition after 12–24 ha | Half Life | Dissociation Velocity from Enzyme | Selectivity versus DPP-8 and DPP-9 | |
|---|---|---|---|---|---|---|
| mg/kg | nM | % | h | sec−1 | fold | |
| Sitagliptin | >30 | 19 | >80 (max. 97) | 8–24 | 50–100,000 | |
| Vildagliptin | 14 | 62 | >80 (max. 95) | 1.5–4.5 | 2.1 × 10−4 | 30–250 |
| Alogliptin | 10 | 24 | 75 (max. 90) | 12–21 | 100,000 | |
| Saxagliptin | 2.7 | 50 | 70 (max. 80) | 2–4 (parent) 3–7 (metabolite) | ||
| Linagliptin (BI 1356) | 0.9 | 1 | 70 (max. 80) | 10–40 | 3.0 × 10−5 | 10,000 |
| Dutogliptin (PHX 1149) | 2.5 | 15–319 |
↵a Degree of inhibition does not translate into dosing.