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. 2017 Oct 5;8(6):1215–1226. doi: 10.1007/s13300-017-0302-3

Table 1.

Comparison between currently available DPP-4 inhibitors

Sitagliptin Saxagliptin Vildagliptin Linagliptin Alogliptin
Dosage 100 mg once daily 5 mg once daily 50 mg twice daily 5 mg once daily 25 mg once daily
Approximate half-life (h) 12 2 3 >120 21
Elimination Metabolism is a minor pathway; primarily eliminated unchanged in urine (75%) Elimination by metabolism (cytochrome P450 3A4/5) and renal clearance (24%) Elimination by metabolism (not CYP450 enzymes) and renal clearance (23%) Enterohepatic; eliminated unchanged in feces via biliary excretion (85%) Metabolism is a minor pathway; primarily eliminated unchanged in urine (63%)
Effect on weight Weight neutral Weight neutral Weight neutral Weight neutral Weight neutral
HbA1c reduction (monotherapy) Clinically important; up to −0.8% Clinically important; up to −0.8% Clinically important; up to −0.8% Clinically important; up to −0.8% Clinically important; up to −0.8%
Use in CKD Reduce dose to 50 mg/day for moderate CKD (CrCl ≥30 to ≤50 mL/min); reduce dose to 25 mg/day for severe CKD (CrCl <30 mL/min); assess renal function before use and on a regular basis Reduce dose to 2.5 mg/day for moderate CKD (CrCl ≥30 to ≤50 mL/min); give reduced dose after dialysis in chronic renal failure Reduce dose to 50 mg/day for moderate CKD (CrCl ≥30 to ≤50 mL/min) and severe CKD (CrCl <30 mL/min) No dosage reduction required Reduce dose to 12.5 mg/day for moderate CKD (CrCl ≥30 to ≤50 mL/min); reduce dose to 6.25 mg/day for severe CKD (CrCl <30 mL/min)
Adverse events Low Low Low Low Low