Assessment of desloratadine as an inhibitor of UGT enzymes in pooled human liver microsomes (HLM) and recombinant enzymes (rUGT)
| UGT enzyme | Substrate | Inhibition by 10 μM Desloratadine (% Activity Remaining) | |
|---|---|---|---|
| HLM | rUGT | ||
| UGT1A1 | 17β-Estradiol | 89.7 | 102 |
| UGT1A3 | CDCA | 92.1 | 90.4 |
| UGT1A4 | Trifluoperazine | 88.3 | 94.7 |
| UGT1A6 | 1-Naphthol | 94.4 | 104 |
| UGT1A9 | Propofol | 103 | 94.1 |
| UGT2B7 | Morphine | 91.2 | 89.4 |
| UGT2B10 | Levomedetomidine | 16.0 | 26.4 |
| UGT2B15 | Oxazepama | 92.4 | 113 |
| UGT2B17 | Testosterone | 75.7 | 61.7 |
| UGT1A7 | 4-Methylumbelliferone | Not applicable | 108 |
| UGT1A8 | 115 | ||
| UGT1A10 | 53.5 | ||
| UGT2B4 | 62.1 | ||
↵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.