Details of the Metabolic Reaction (MR)

General Information of This Metabolic Reaction (MR) (ID: MR002971)
Formula Reactant Aprepitant Product (2R)-2-(4-fluorophenyl)-2-{[(5-oxo-2,5-dihydro-1H-1,2,4-triazol-3-yl)methyl]amino}acetic acid
Reactant Info Product Info
Metabolic Enzyme Cytochrome P450 3A4 (CYP3A4) DME Info
Cytochrome P450 1A2 (CYP1A2) DME Info
Mephenytoin 4-hydroxylase (CYP2C19) DME Info
Metabolic Type Oxidation - O-Dealkylation
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
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]
MR002975 Aprepitant Aprepitant glucuronide Conjugation - Glucuronidation Aprepitant [3]
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.
3 In vitro glucuronidation of aprepitant: a moderate inhibitor of UGT2B7 Xenobiotica. 2015;45(11):990-8. doi: 10.3109/00498254.2015.1038743.

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