Details of the Metabolic Reaction (MR)

General Information of This Metabolic Reaction (MR) (ID: MR000768)
Formula
UGT1A1 ...
SVG example
Glucuronidation
Reactant 3-hydroxydesloratadine Product 3-hydroxydesloratadine O-glucuronide
Reactant Info Product Info
Metabolic Enzyme UDP-glucuronosyltransferase 1A1 (UGT1A1) DME Info
UDP-glucuronosyltransferase 1A3 (UGT1A3) DME Info
UDP-glucuronosyltransferase 2B15 (UGT2B15) DME Info
Metabolic Type Conjugation - Glucuronidation
Other MR(s) Related to The Reactant of This MR
Other MR(s) That Produce The Reactant of This MR
MR ID Reactant Product MR Type Related Drug REF
MR005248 Rupatadine 3-hydroxydesloratadine Unclear Rupatadine [1]
MR006902 Desloratadine glucuronide 3-Hydroxydesloratadine Oxidation - 3-hydroxylation Loratadine [2]
MR000767 3-hydroxydesloratadine N-glucuronide 3-hydroxydesloratadine Unclear Desloratadine [3], [4]
References
1 CYP3A5*3 and MDR1 C3435T are influencing factors of inter-subject variability in rupatadine pharmacokinetics in healthy Chinese volunteers. Eur J Drug Metab Pharmacokinet. 2016 Apr;41(2):117-24.
2 Advances in high-resolution MS and hepatocyte models solve a long-standing metabolism challenge: the loratadine story. Bioanalysis. 2016 Aug;8(16):1645-62.
3 Further characterization of the metabolism of desloratadine and its cytochrome P450 and UDP-glucuronosyltransferase inhibition potential: identification of desloratadine as a relatively selective UGT2B10 inhibitor. Drug Metab Dispos. 2015 Sep;43(9):1294-302.
4 A long-standing mystery solved: the formation of 3-hydroxydesloratadine is catalyzed by CYP2C8 but prior glucuronidation of desloratadine by UDP-glucuronosyltransferase 2B10 is an obligatory requirement Drug Metab Dispos. 2015 Apr;43(4):523-33. doi: 10.1124/dmd.114.062620.

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