TABLE 2

AUC0–48h, AUCinf, and T1/2 of icenticaftor and its metabolites in plasma based on metabolite pattern analysis

PeakaCompound/
metabolite
AUC0–48h
(nmol*h/L)
Percentage
AUC0–48h
AUCinf
(nmol*h/L)
Percentage AUCinfT1/2
(h)
M5O-demethylation, glucuronidation1280010.71380010.712.1
M8N-glucuronidation4220035.34410033.911.2
M9O-glucuronidation1730014.51810013.911.6
M10C-hydroxylation23101.9328402.19
M14O-demethylation17901.5020001.5416.8
M17N-dealkylation36303.0438402.9610.7
IcenticaftorParent drug2210018.522700b17.511.2
Sum of minor identified metabolites (each ≤1%)79306.63
Sum of unknown trace metabolites (each ≤0.30%)5150.430
Lost during sample processing and HPLC88707.42
Total 14C (total of radiolabeled components)12000010013000010014.2
  • –, not calculated; AUC0–48h, area under the concentration-time curve from time zero to 48 hours.

  • aListed in order of elution.

  • b8200 ng*h/ml.