TABLE 4

Metabolite pattern in plasma, urine, and feces after a single intravenous dose of 5 mg (10.6 μmol) of [14C]linagliptin (arithmetic means of six individuals)

MetabolitePlasmaUrine (0–48 h)Feces (0–240 h)Urine + Feces (Total)
1.5 h3 + 6 h
% of sample radioactivity% of dose
Linagliptin93.583.925.335.861.1
CD17905.610.90.12.52.6
M489(1)0.70.39.39.6
M503(1)0.21.21.4
M506(1)4.04.0
M665(3)1.2
M665(8)+M650(1)0.92.7
m4*0.6
Others (sum)1.6**0.31.9**
Total100.0100.027.553.280.7
  • Empty cells, not detected.

  • * Not assigned to metabolite structure(s).

  • ** Individually ≤0.7%.