TABLE 5

Metabolite pattern in plasma, urine, and feces after a single oral dose of 10 mg (21.2 μmol) of [14C]linagliptin (arithmetic means of six individuals)

MetabolitePlasma (1.5 h + 3 + 6 h)Urine (0–48 h)Feces (0–120 h)Urine + Feces (Total)
% of sample radioactivity% of dose
Linagliptin74.23.974.178.0
CD179016.90.20.30.5
M489(1)0.30.24.54.7
M531(1)+M490(1)+ M506(1)2.52.5
M665(3)
M665(8)+M650(1)5.5
m4*3.1
Others (sum)1.1**0.11.3**
Total100.05.481.587.0
  • Empty cells, not detected.

  • * Not assigned to metabolite structure(s).

  • ** Individually ≤0.3%.