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

Desloratadine (Clarinex), the major active metabolite of loratadine (Claritin), is a nonsedating long-lasting antihistamine that is widely used for the treatment of allergic rhinitis and chronic idiopathic urticaria. For over 20 years, it has remained a mystery as to which enzymes are responsible fo...

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Veröffentlicht in:	Drug metabolism and disposition 2015-04, Vol.43 (4), p.523-533
Hauptverfasser:	Kazmi, Faraz, Barbara, Joanna E, Yerino, Phyllis, Parkinson, Andrew
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Aryl Hydrocarbon Hydroxylases - genetics Aryl Hydrocarbon Hydroxylases - metabolism Biocatalysis Cells, Cultured Cryopreservation Cytochrome P-450 CYP2C8 - genetics Cytochrome P-450 CYP2C8 - metabolism Dogs Enzyme Inhibitors - pharmacology Glucuronides - metabolism Glucuronosyltransferase - antagonists & inhibitors Glucuronosyltransferase - genetics Glucuronosyltransferase - metabolism Haplorhini Hepatocytes - drug effects Hepatocytes - enzymology Hepatocytes - metabolism Humans Loratadine - analogs & derivatives Loratadine - metabolism Loratadine - pharmacokinetics Mice Microsomes, Liver - drug effects Microsomes, Liver - enzymology Microsomes, Liver - metabolism Rabbits Rats Recombinant Proteins Species Specificity Swine Swine, Miniature
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