TABLE 3

Assessment of desloratadine as an inhibitor of UGT enzymes in pooled human liver microsomes (HLM) and recombinant enzymes (rUGT)

UGT enzymeSubstrateInhibition by 10 μM Desloratadine (% Activity Remaining)
HLMrUGT
UGT1A117β-Estradiol89.7102
UGT1A3CDCA92.190.4
UGT1A4Trifluoperazine88.394.7
UGT1A61-Naphthol94.4104
UGT1A9Propofol10394.1
UGT2B7Morphine91.289.4
UGT2B10Levomedetomidine16.026.4
UGT2B15Oxazepama92.4113
UGT2B17Testosterone75.761.7
UGT1A74-MethylumbelliferoneNot applicable108
UGT1A8115
UGT1A1053.5
UGT2B462.1
  • a Racemic oxazepam was used as the substrate; however, only S-oxazepam glucuronide was monitored by LC-MS/MS.

  • CDCA, chenodeoxycholic acid; HLM, human liver microsomes; rUGT, recombinant UDP-glucuronsyltransferase.