Details of the Metabolic Reaction (MR)

General Information of This Metabolic Reaction (MR) (ID: MR005248)
Formula
SVG example
Reactant Rupatadine Product 3-hydroxydesloratadine
Reactant Info Product Info
Metabolic Enzyme Cytochrome P450 3A4 (CYP3A4) DME Info
Other MR(s) Related to The Reactant of This MR
Other MR(s) That Metabolize The Reactant of This MR
MR ID Reactant Product MR Type Related Drug REF
MR005247 Rupatadine Desloratadine Unclear Rupatadine [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
MR006902 Desloratadine glucuronide 3-Hydroxydesloratadine Oxidation - 3-hydroxylation Loratadine [2]
MR000767 3-hydroxydesloratadine N-glucuronide 3-hydroxydesloratadine Unclear Desloratadine [3], [4]
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 [2]
MR000768 3-hydroxydesloratadine 3-hydroxydesloratadine O-glucuronide Conjugation - Glucuronidation Desloratadine [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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