Linagliptin

DPP-4 inhibitor, Antihyperglycemic agent, Incretin pathway modulator

Linagliptin

Tradjenta; with metformin Jentadueto

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Summary

Classes

DPP-4 inhibitor, Antihyperglycemic agent, Incretin pathway modulator

Common uses

Type 2 diabetes mellitus▲0▼

Pharmacy

Starting dose

5 mg PO once daily (no renal dose adjustment, unlike sitagliptin)

Preparations

5 mg tablets; combination with metformin

US FDA Max

5 mg/d

Pharmacology

Routes

Oral

Onset

Postprandial glucose effect within days; HbA1c by 12 weeks

Duration

24 hours

Half-life

~12 hours (effective); terminal much longer

Bioavailability

~30% (oral)

Pregnancy

Limited data; switch to insulin where feasible.^{[citation needed]}

Legal status

Rx-only in US

Purported mechanism

Linagliptin reversibly inhibits dipeptidyl peptidase-4 (DPP-4), extending the half-life of the endogenous incretins GLP-1 and GIP; the resulting glucose-dependent increase in insulin secretion and decrease in glucagon lowers fasting and postprandial glucose without significant hypoglycemia risk as monotherapy.▲0▼ Unlike other gliptins, linagliptin is predominantly biliary-cleared rather than renal, making it the only DPP-4 inhibitor that does not require dose adjustment in CKD — its clinical niche. Class adverse effects (pancreatitis signal, severe joint pain, bullous pemphigoid) apply.