Details of the Metabolic Reaction (MR)

General Information of This Metabolic Reaction (MR) (ID: MR006902)
Formula Reactant Desloratadine glucuronide Product 3-Hydroxydesloratadine
Reactant Info Product Info
Metabolic Enzyme Cytochrome P450 2C8 (CYP2C8) DME Info
Metabolic Type Oxidation - 3-hydroxylation
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
MR006904 Desloratadine Desloratadine glucuronide Conjugation - Glucuronidation Loratadine [1]
Other MR(s) Related to The Product of This MR
Other MR(s) That Produce The Product of This MR
MR ID Reactant Product MR Type Related Drug REF
MR005248 Rupatadine 3-hydroxydesloratadine Unclear Rupatadine [2]
MR000767 3-hydroxydesloratadine N-glucuronide 3-hydroxydesloratadine Unclear Desloratadine [3], [1]
Other MR(s) That Metabolize The Produtc of This MR
MR ID Reactant Product MR Type Related Drug REF
MR006903 3-Hydroxydesloratadine 3-hydroxydesloratadine O-glucuronide Conjugation - Glucuronidation Loratadine [4]
MR000768 3-hydroxydesloratadine 3-hydroxydesloratadine O-glucuronide Conjugation - Glucuronidation Desloratadine [1]
References
1 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.
2 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.
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 Advances in high-resolution MS and hepatocyte models solve a long-standing metabolism challenge: the loratadine story. Bioanalysis. 2016 Aug;8(16):1645-62.

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