Table 2.
Selected pharmacodynamic and pharmacokinetic properties of gliptins evaluated in cancer studies [21,22,23,24,25].
| Generic Name | Daily Dose (mg) Used in Diabetic Patients | IC50 DPP-IV (nM) | IC50 DPP8 (nM) | IC50 DPP9 (nM) | IC50 FAP (nM) | Cmax (nM) in Humans |
|---|---|---|---|---|---|---|
| Gemigliptin | 50 | 6.3 | 277,000 | 233,000 | 418,430 | 128 |
| Sitagliptin | 100 | 19 | 48,000 | >100,000 | >500,000 | 959 |
| Vildagliptin | 100 (2 × 50) | 3 | 810 | 95 | 54,600 | 1309 |
| Saxagliptin | 5 | 1.3 | 520 | 98 | >1000 | 76 |
| Linagliptin | 5 | 1 | >100,000 | >100,000 | 89 | 10 |
| Alogliptin | 25 | 6.9 | >100,000 | >100,000 | >500,000 | 324 |
| Teneligliptin | 20 | 0.37 | 260 | 540 | >10,000 | 645 |
| Anagliptin | 200 (2 × 100) | 3.8 | 63,000 | 60,000 | 72,700 | 1242 |