What is the recommended dosing for Tenelegliptin (Dipeptidyl peptidase-4 inhibitor) in patients with Impaired renal function?

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—the standard dose of 20 mg once daily can be safely administered across all stages of chronic kidney disease. 1

Standard Dosing Across All Renal Function Levels

Teneligliptin 20 mg once daily is the recommended dose regardless of eGFR, from normal renal function through end-stage renal disease. 1, 2 This represents a significant clinical advantage over most other DPP-4 inhibitors, which require dose reductions as renal function declines. 1

Pharmacokinetic Rationale

• Pharmacokinetic studies demonstrate that while AUC increases in patients with renal impairment, this increase is unrelated to the degree of renal dysfunction and does not necessitate dose adjustment. 2
• Maximum plasma concentration (Cmax) remains unchanged across all stages of renal impairment following a 20 mg dose. 2
• Plasma protein binding remains <80% in all patient groups, including those with end-stage renal disease. 2
• Dialysis does not significantly affect teneligliptin pharmacokinetics, so no dose adjustment is needed for hemodialysis patients. 2

Clinical Evidence Supporting No Dose Adjustment

End-Stage Renal Disease Data

• A prospective study in hemodialysis patients demonstrated that teneligliptin 20 mg once daily significantly improved glycemic control with blood glucose decreasing by 36.7 mg/dL at 4 weeks (p < 0.05). 3
• Glycated albumin decreased by 3.1% at 28 weeks compared to controls (p < 0.05) in dialysis patients receiving standard 20 mg dosing. 3
• No cases of hypoglycemia occurred in hemodialysis patients treated with teneligliptin 20 mg daily. 3
• The medication was well tolerated with no treatment discontinuations due to adverse effects in the end-stage renal disease population. 3

Optimal Dosing Regimen

For maximum glycemic efficacy, teneligliptin 40 mg once daily may be considered, as it demonstrates superior HbA1c reduction compared to 20 mg without compromising safety. 4

• The 40 mg dose showed the highest probability of achieving HbA1c <7% (SUCRA 85.81%) among all studied interventions. 4
• Both 20 mg and 40 mg doses demonstrated acceptable safety profiles with no significant increase in hypoglycemia risk compared to placebo. 4
• The antidiabetic effect gradually increases from 5 mg to 40 mg, with 40 mg considered the optimal dosage for efficacy while maintaining safety. 4

Comparison with Other DPP-4 Inhibitors Requiring Dose Adjustment

Teneligliptin's lack of required dose adjustment distinguishes it from most other DPP-4 inhibitors, which require significant dose reductions in renal impairment. 5, 1

Dose Adjustments Required for Alternative DPP-4 Inhibitors:

• Sitagliptin: 50 mg daily when eGFR 30-44 mL/min/1.73 m²; 25 mg daily when eGFR <30 mL/min/1.73 m² (compared to standard 100 mg). 5, 1
• Saxagliptin: Maximum 2.5 mg daily when eGFR ≤45 mL/min/1.73 m² (compared to standard 5 mg). 5, 1
• Alogliptin: 12.5 mg daily when eGFR 30-60 mL/min/1.73 m²; 6.25 mg daily when eGFR <30 mL/min/1.73 m² (compared to standard 25 mg). 5, 1
• Linagliptin: Like teneligliptin, requires no dose adjustment across all stages of renal impairment. 5, 1

Important Clinical Context and Limitations

DPP-4 inhibitors, including teneligliptin, should not be first-line therapy for patients with established atherosclerotic cardiovascular disease, heart failure, or chronic kidney disease with albuminuria. 1, 6

• In these high-risk populations, GLP-1 receptor agonists or SGLT2 inhibitors are strongly preferred due to proven cardiovascular and renal benefits. 5, 1
• DPP-4 inhibitors have demonstrated cardiovascular safety but no cardiovascular benefit in outcome trials. 6
• The glucose-lowering efficacy of DPP-4 inhibitors is moderate (HbA1c reduction 0.4-0.9%), less potent than GLP-1 receptor agonists or SGLT2 inhibitors. 6

Monitoring Recommendations

• Assess HbA1c every 3 months to determine treatment efficacy. 1
• Monitor renal function periodically as part of routine diabetes care, though this does not necessitate dose changes for teneligliptin. 1
• No specific safety monitoring beyond standard diabetes care is required, as teneligliptin maintains a favorable safety profile across all stages of kidney disease. 1

Common Pitfalls to Avoid

• Do not reduce teneligliptin dose based on declining renal function—this is unnecessary and may result in suboptimal glycemic control. 1, 2
• Do not use teneligliptin as first-line therapy in patients with established cardiovascular disease or heart failure—these patients benefit more from SGLT2 inhibitors or GLP-1 receptor agonists. 1
• Do not assume all DPP-4 inhibitors have the same renal dosing requirements—only linagliptin and teneligliptin require no dose adjustment. 5, 1