Details of the Metabolic Reaction (MR)

General Information of This Metabolic Reaction (MR) (ID: MR002975)
Formula Reactant Aprepitant Product Aprepitant glucuronide
Reactant Info Product Info
Metabolic Enzyme UDP-glucuronosyltransferase 1A4 (UGT1A4) DME Info
Metabolic Type Conjugation - Glucuronidation
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
MR002971 Aprepitant (2R)-2-(4-fluorophenyl)-2-{[(5-oxo-2,5-dihydro-1H-1,2,4-triazol-3-yl)methyl]amino}acetic acid Oxidation - O-Dealkylation Aprepitant [1], [2]
MR002969 Aprepitant (2S,3R)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholine Oxidation - N-Dealkylation Aprepitant [1], [2]
MR002973 Aprepitant 1-[3,5-bis(trifluoromethyl)phenyl]ethanone Oxidation - N-Demethylation Aprepitant [1], [2]
MR002970 Aprepitant 5-({[(1R)-1-(4-fluorophenyl)-2-hydroxyethyl]amino}methyl)-2,3-dihydro-1H-1,2,4-triazol-3-one Oxidation - O-Dealkylation Aprepitant [1], [2]
MR002972 Aprepitant 5-oxo-1,4-dihydro-1,2,4-triazole-3-carbaldehyde Oxidation - N-Dealkylation Aprepitant [1], [2]
MR002974 Aprepitant 5-{[(2S,3S)-3-(4-fluorophenyl)-2-hydroxymorpholin-4-yl]methyl}-2,4-dihydro-1,2,4-triazol-3-one Oxidation - N-Demethylation Aprepitant [1], [2]
References
1 Cytochrome P450 3A4 is the major enzyme involved in the metabolism of the substance P receptor antagonist aprepitant. Drug Metab Dispos. 2004 Nov;32(11):1287-92.
2 Lack of effect of aprepitant on the pharmacokinetics of docetaxel in cancer patients. Cancer Chemother Pharmacol. 2005 Jun;55(6):609-16.

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