Table 2

Metabolic profile of tresperimus after incubation in rat and human plasma for 6 h at 37°C

Incubation TimeSpeciesQuantitative Analysis TresperimusStructural Analysis
TresperimusM1M3M4M6
h μM metabolite area/internal standard area
0Human7.71715.400<LOD<LOD<LOD<LOD
Rat7.68516.010<LOD<LOD<LOD<LOD
2Human6.60412.6000.2250.8100.029<LOD
Rat5.63611.3200.0200.0260.0090.630
4Human5.46210.4000.1782.210.129<LOD
Rat4.1798.0400.0080.0490.0130.860
6Human4.4698.5500.1163.340.332<LOD
Rat3.4806.5000.0080.0980.0170.810

Tresperimus disappearance was quantified in duplicate by HPLC analysis. Values are means (n = 2). Plasma of each species was collected and pooled at each incubation time for the structural analysis performed by LC/MS.

  • LOD, limit of detection.