General Information of DME (ID: DMEN075)
DME Name Flavin-containing monooxygenase (FMO), .
Gene Name FMO
      Click to Show/Hide the Molecular/Functional Data (Sequence/Structure/Pathway/Function) of This DME
Full List of Drug(s) Metabolized by This DME
      Drugs Approved by FDA Click to Show/Hide the Full List of Drugs:          4 Drugs
Fingolimod
Drug Info Approved Multiple sclerosis ICD11: 8A40 [1]
Fingolimod hydrochloride
Drug Info Approved Multiple sclerosis ICD11: 8A40 [1]
Loxapine succinate
Drug Info Approved Schizophrenia ICD11: 6A20 [2]
Guanethidine
Drug Info Approved Essential hypertension ICD11: BA00 [3]
      Drugs in Phase 3 Clinical Trial Click to Show/Hide the Full List of Drugs:          1 Drugs
NE-10064
Drug Info Phase 3 Cardiac arrhythmia ICD11: BC65 [4]
      Drugs in Phase 2 Clinical Trial Click to Show/Hide the Full List of Drugs:          3 Drugs
PD-115934
Drug Info Phase 2 Breast cancer ICD11: 2C60 [5]
ASA-404
Drug Info Phase 2 Prostate cancer ICD11: 2C82 [6], [7]
E7016
Drug Info Phase 2 Melanoma ICD11: 2C30 [8]
      Discontinued/withdrawn Drugs Click to Show/Hide the Full List of Drugs:          1 Drugs
ABT-418
Drug Info Discontinued in Phase 2 Alzheimer disease ICD11: 8A20 [9]
      Preclinical/investigative Agents Click to Show/Hide the Full List of Drugs:          1 Drugs
Fenthion
Drug Info Investigative Discovery agent ICD: N.A. [10]
Full List of Metabolic Reactions (MR) Catalyzed by This DME
MR ID Reactant Product MR Type Source Drug REF
MR010063 ABT-418 ABT-418 Metabolite M2 Unclear - Unclear ABT-418 [11], [9]
MR000105 (+) albendazole sulfoxide Albendazole sulfone Oxidation - Oxidation Albendazole [12], [13], [14]
MR000109 Albendazole (+) albendazole sulfoxide Oxidation - Oxidation Albendazole [15], [12], [13], [14]
MR007274 ASA-404 6-OH-MXAA Unclear - Unclear ASA-404 [6], [7]
MR013843 Ketone Lactone Unclear - Unclear E7016 [8]
MR006302 Fenthion FEN-sulfoxide Unclear - Unclear Fenthion [10]
MR006306 Fenthion oxon Fenthion oxon sulfoxide Unclear - Unclear Fenthion [10]
MR008792 Guanethidine Guanethidine N-oxide Unclear - Unclear Guanethidine [3]
MR011379 LEE011 LEE011 Metabolite M13 Unclear - Unclear LEE011 [16]
MR006925 Loxapine succinate Loxapine N-oxide Oxidation - Oxidationn Loxapine succinate [2]
MR013813 Methimazole M9 Methimazole M10 Unclear - Unclear Methimazole [17]
MR003787 NE-10064 NE-10064 Metabolite M5 Unclear - Unclear NE-10064 [4]
MR003783 NE-10064 NE-10064 Metabolite M4 Oxidation - N-oxidation NE-10064 [4]
MR002343 Tazarotenic acid AGN 190844 Oxidation - Oxidation Tazarotene [18], [19], [20]
⏷ Show the Full List of 14 MR(s)
References
1 CYP4F enzymes are responsible for the elimination of fingolimod (FTY720), a novel treatment of relapsing multiple sclerosis. Drug Metab Dispos. 2011 Feb;39(2):191-8.
2 In vitro identification of the human cytochrome p450 enzymes involved in the oxidative metabolism of loxapine. Biopharm Drug Dispos. 2011 Oct;32(7):398-407.
3 Guanethidine N-oxide formation as a measure of cellular flavin-containing monooxygenase activity
4 The metabolic profile of azimilide in man: in vivo and in vitro evaluations. J Pharm Sci. 2005 Sep;94(9):2084-95.
5 The metabolism of pyrazoloacridine (NSC 366140) by cytochromes p450 and flavin monooxygenase in human liver microsomes. Clin Cancer Res. 2004 Feb 15;10(4):1471-80.
6 Predicting pharmacokinetics and drug interactions in patients from in vitro and in vivo models: the experience with 5,6-dimethylxanthenone-4-acetic acid (DMXAA), an anti-cancer drug eliminated mainly by conjugation. Drug Metab Rev. 2002 Nov;34(4):751-90.
7 Preclinical factors affecting the interindividual variability in the clearance of the investigational anti-cancer drug 5,6-dimethylxanthenone-4-acetic acid. Biochem Pharmacol. 2003 Jun 1;65(11):1853-65.
8 A Baeyer-Villiger oxidation specifically catalyzed by human flavin-containing monooxygenase 5
9 In vitro hepatic metabolism of ABT-418 in chimpanzee (Pan troglodytes). A unique pattern of microsomal flavin-containing monooxygenase-dependent stereoselective N'-oxidation
10 The participation of human hepatic P450 isoforms, flavin-containing monooxygenases and aldehyde oxidase in the biotransformation of the insecticide fenthion. Toxicol Appl Pharmacol. 2008 Dec 1;233(2):343-52.
11 The in vitro hepatic metabolism of ABT-418, a cholinergic channel activator, in rats, dogs, cynomolgus monkeys, and humans
12 Nanocrystal Suspensions for Enhancing the Oral Absorption of Albendazole. Nanomaterials (Basel). 2022 Sep 1;12(17):3032. doi: 10.3390/nano12173032.
13 Multi-residue methodology for quantification of antiparasitics in hen eggs by LC-MS/MS: development, validation and application to 348 samples from Brazil. Food Addit Contam Part A Chem Anal Control Expo Risk Assess. 2022 Aug;39(8):1412-1423. doi: 10.1080/19440049.2022.2093984.
14 Improvement of Albendazole Bioavailability with Menbutone Administration in Sheep. Animals (Basel). 2022 Feb 14;12(4):463. doi: 10.3390/ani12040463.
15 Hardman, J.G., L.E. Limbird, P.B., A.G. Gilman. Goodman and Gilman's The Pharmacological Basis of Therapeutics. 10th ed. New York, NY:McGraw-Hill, 2001., p. 1126
16 An integrated assessment of the ADME properties of the CDK4/6 Inhibitor ribociclib utilizing preclinical in vitro, in vivo, and human ADME data
17 Evidence for the involvement of N-methylthiourea, a ring cleavage metabolite, in the hepatotoxicity of methimazole in glutathione-depleted mice: structure-toxicity and metabolic studies
18 Clinical pharmacokinetics and drug metabolism of tazarotene: a novel topical treatment for acne and psoriasis Clin Pharmacokinet. 1999 Oct;37(4):273-87. doi: 10.2165/00003088-199937040-00001.
19 Cytochrome P450 2C8 and flavin-containing monooxygenases are involved in the metabolism of tazarotenic acid in humans. Drug Metab Dispos. 2003 Apr;31(4):476-81.
20 LABEL:AZAROTENE aerosol, foam

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