TABLE 2

Plasma concentrations and PK parameters of tropifexor and its metabolites after a single oral dose of 1 mg [14C]tropifexor to healthy subjects

Time (h)M11.6aM22.4aTropifexora
10.0773b1.74
20.3710.24013.1
40.8321.0935.1
60.4831.0127.5
80.3631.3726.7
120.3081.1819.0
240.4127.45
480.1500.2492.17
720.987
Cmax (ng-eq/ml)0.8321.3735.1
Tmax (h)484
AUC0–72hc (h*ng-eq/ml)10.431.5576
AUCinf (h*ng-eq/ml)NCdNC597
%Total radioactivity AUC0–72he1.655.0091.6
%Parent AUC0–72h1.815.46100
  • aThe plasma radioactivity concentrations are expressed in ng-eq/ml.

  • bNot detected.

  • cCalculated using linear trapezoidal method. The concentrations at time 0 was taken as zero.

  • dNot calculated.

  • eThe %total radioactivity AUC for each metabolite is calculated based on the total plasma radioactivity AUC0-72h of 629 h*ng-eq/ml.