|
| Teneligliptin | Sitagliptin | Vildagliptin | Saxagliptin | Alogliptin | Linagliptin | |||
| Absorption | |||||||||
| Route | Oral | Oral | Oral | Oral | Oral | Oral | |||
| Bioavailability | 63% - 85% | 87% | 85% | 67% | 100% | 30% | |||
| Tmax | 1.33 h | 1 to 4 h | 1.75 h | 2 h | 1 - 2 h | 1.5 h | |||
| Effect of food | No | No | No | No | No | No | |||
| Distribution | |||||||||
| Protein Binding | 78% - 80% | 38% | 9.3% | Negligible | 20% | 70% - 80% | |||
| Metabolism | |||||||||
| CYP | CYP3A4 & FMO 1 & 3 | Minor CYP3A4, CYP2C8 | Minor (~57% of administered drug catabolized by non-CYP-mediated hydrolysis to an inactive metabolite, LAY151) | CYP P450 3A4/5 | Minor CYP2D6, CYP3A4 | Not metabolized by CYP
| |||
| Metabolites | Inactive | Inactive | Inactive | Active (BMS-510849) | Inactive | Inactive | |||
| Excretion | |||||||||
| T1/2 (hours [hr]) | 26.9 hr | 2 - 3 hr | 3 hr | 2.5 hr Metabolite 3.1 hr | 21 hr | >100 hr | |||
| Clearance (%) | Feces (46.5%) Urine (45.4%) | Feces (13%) Urine (87%) | Feces (15%) Urine (85%) | Feces (22%) Urine (78%) | Feces (13%) Urine (76%) | Feces (85%) Urine (5%) | |||
| Drug-Drug interactions | No major clinically relevant drug-drug interactions | Plasma AUC of digoxin was increased by 11%, otherwise no major interaction reported | Low potential for drug interaction | Caution?with drugs metabolized by CYP3A4/5 system (Atazanavir, Clarithromycin, Indinavir, Itraconazole, Ketoconazole, Nefazodone, Nelfinavir, Ritonavir, Saquinavir, Telithromycin) | No significant drug-drug interactions | Rifampin | |||