Teneligliptin Dosing in Renal Impairment
Teneligliptin does not require dose adjustment in patients with any degree of renal impairment, including end-stage renal disease requiring hemodialysis. 1, 2, 3
Standard Dosing Across All Renal Function Levels
- Administer 20 mg once daily regardless of estimated glomerular filtration rate (eGFR) or creatinine clearance. 2, 3, 4
- This recommendation applies to all stages of chronic kidney disease, including patients on hemodialysis. 1, 4
- The standard dose remains 20 mg once daily even in severe renal impairment (eGFR <30 mL/min/1.73 m²). 1, 3
Pharmacokinetic Rationale
Teneligliptin's unique elimination profile distinguishes it from most other DPP-4 inhibitors:
- Multiple elimination pathways: Teneligliptin is eliminated through three distinct routes: renal excretion (unchanged), metabolism by cytochrome P450 3A4 (CYP3A4), and metabolism by flavin-containing monooxygenase 3 (FMO3). 2, 3
- This redundancy in elimination pathways prevents drug accumulation when renal function declines. 3
- The half-life is approximately 24 hours, providing sustained DPP-4 inhibition throughout the day. 2, 3
Comparison with Other DPP-4 Inhibitors
Understanding the dosing requirements of alternative DPP-4 inhibitors helps contextualize teneligliptin's advantage in renal impairment:
Agents Requiring Dose Adjustment:
- Sitagliptin: Requires dose reduction when eGFR <45 mL/min/1.73 m² (100 mg daily if eGFR ≥45; 50 mg daily if eGFR 30-44; 25 mg daily if eGFR <30). 5, 1
- Saxagliptin: Requires dose reduction when eGFR ≤45 mL/min/1.73 m² (maximum 2.5 mg daily). 5, 6
- Alogliptin: Requires dose adjustment based on renal function (25 mg if eGFR >60; 12.5 mg if eGFR 30-60; 6.25 mg if eGFR <30). 5
Agents Not Requiring Dose Adjustment:
- Linagliptin: Like teneligliptin, requires no dose adjustment in any degree of renal impairment (5 mg daily regardless of eGFR). 5, 1
- Vildagliptin: Does not require dose adjustment in renal impairment. 7
Clinical Evidence in Renal Impairment
- A prospective study in hemodialysis patients demonstrated that teneligliptin 20 mg once daily significantly improved glycemic control without requiring dose adjustment. 4
- Blood glucose decreased by 36.7 mg/dL from 4 weeks of treatment, with glycated albumin decreasing by 3.1% at 28 weeks. 4
- A randomized crossover study comparing teneligliptin 20 mg daily with linagliptin 5 mg daily in type 2 diabetes patients with CKD (eGFR <60 mL/min/1.73 m²) showed comparable efficacy for glycemic control. 8
Safety Profile
- No hypoglycemia was observed in clinical studies of teneligliptin in patients with end-stage renal disease on hemodialysis. 4
- The American Diabetes Association and National Kidney Foundation indicate that teneligliptin maintains a favorable safety profile across all stages of kidney disease. 1
- The incidence of adverse drug reactions is approximately 10% across all clinical studies, with hypoglycemia rates comparable to placebo. 2
- No serious hypoglycemia has been reported in clinical trials. 2
Important Clinical Caveats
- General DPP-4 inhibitor limitations: While teneligliptin offers dosing convenience in renal impairment, DPP-4 inhibitors as a class should not be first-line therapy for patients with established atherosclerotic cardiovascular disease, heart failure, or chronic kidney disease with albuminuria—in these populations, GLP-1 receptor agonists or SGLT2 inhibitors are preferred due to proven cardiovascular and renal benefits. 5
- Pancreatitis risk: Although causality has not been established, acute pancreatitis has been reported with DPP-4 inhibitors; discontinue if pancreatitis is suspected. 5
- Heart failure considerations: Unlike saxagliptin and alogliptin, teneligliptin has not been associated with increased heart failure risk, but monitor for signs and symptoms of heart failure in at-risk patients. 5