General Information of DME (ID: DEJVYAZ)

DME Name Cytochrome P450 2A6 (CYP2A6) DME Info
Gene Name CYP2A6

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Investigative Drug(s)
48 Approved Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [1]
Apremilast DMTWS9E Psoriasis vulgaris EA90 Approved [2]
Arformoterol DMYM974 Chronic obstructive pulmonary disease CA22 Approved [3]
Artemisinin DMOY7W3 Malaria 1F40-1F45 Approved [4]
Artesunate DMR27C8 Infection of P. falciparum 1F40 Approved [5]
Azelastine DMXTMBJ Allergic conjunctivitis 9A60.02 Approved [6]
Camphor DMWIO46 Acute or chronic pain MG30-MG31 Approved [7]
Cenobamate DM8KLU9 Complex partial seizure 8A68.0 Approved [8]
Chlorzoxazone DMCYVDT Acute pain MG31 Approved [9]
Cinnarizine DM7U5QJ Meniere disease AB31.0 Approved [10]
Cisapride DMY7PED Gastroesophageal reflux disease DA22.Z Approved [11]
Clofibrate DMPC1J7 Dysbetalipoproteinemia 5C80.2 Approved [12]
Clozapine DMFC71L Schizophrenia 6A20 Approved [13]
Cyclophosphamide DM4O2Z7 Advanced cancer 2A00-2F9Z Approved [14]
Dapagliflozin DM28UJG Non-insulin dependent diabetes 5A11 Approved [15]
Dexmedetomidine DM93L4X Irritability MB24 Approved [16]
Flunarizine DMZU5JP Migraine 8A80 Approved [12]
Flunitrazepam DMGR5Z3 Insomnia 7A00-7A0Z Approved [17]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [18]
Flurazepam DMAL4G0 Insomnia 7A00-7A0Z Approved [19]
Halothane DM80OZ5 Anaesthesia 9A78.6 Approved [20]
Ifosfamide DMCT3I8 Adult central nervous system germ cell tumor Approved [21]
Letrozole DMH07Y3 Estrogen-receptor positive breast cancer Approved [22]
Lidocaine DML4ZOT Anaesthesia 9A78.6 Approved [23]
Lorcaserin DMG6OYJ Obesity 5B81 Approved [24]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [25]
Methoxsalen DME8FZ9 Cutaneous T-cell lymphoma 2B01 Approved [4]
Methoxyflurane DML0RAE Anaesthesia 9A78.6 Approved [26]
Metronidazole DMTIVEN Abscess Approved [27]
Montelukast DMD157S Allergic asthma CA23.0 Approved [10]
Nevirapine DM6HX9B Human immunodeficiency virus infection 1C62 Approved [10]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [28]
Norethindrone acetate DMDGCQP N. A. N. A. Approved [29]
Perazine DM2AOTZ Psychotic disorder 6A20-6A25 Approved [30]
Pilocarpine DMV9ADG Glaucoma/ocular hypertension 9C61 Approved [31]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [23]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [32]
Selegiline Hydrochloride DM3VR1L Parkinson disease 8A00.0 Approved [33]
Sevoflurane DMC9O43 Anaesthesia 9A78.6 Approved [26]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [34]
Tegafur DM31ZQM Solid tumour/cancer 2A00-2F9Z Approved [35]
Thalidomide DM70BU5 Adult T-cell leukemia/lymphoma Approved [36]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [23]
UFT DMX3O0D Solid tumour/cancer 2A00-2F9Z Approved [37]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [38]
Vortioxetine DM6F1PU Major depressive disorder 6A70.3 Approved [39]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [23]
Medifoxamine DM0UGYX N. A. N. A. Phase 4 [23]
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⏷ Show the Full List of 48 Approved Drug(s)
5 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
5-methoxypsoralen DME2A8X Psoriasis vulgaris EA90 Phase 3 [40]
Clomethiazole DMSPN58 Stroke 8B20 Phase 3 [23]
Plitidepsin DMJ8AUE Multiple myeloma 2A83 Phase 3 [41]
BMS 650032 DMQI43G Hepatitis C virus infection 1E51.1 Phase 2 [42]
Roxatidine DMIZMYQ N. A. N. A. Phase 2 [43]
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1 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Phenacetin DMRQAM0 Analgesia MB40.8 Withdrawn from market [44]
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7 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Chloroxylenol DMM75WZ N. A. N. A. Investigative [23]
Fenthion DMKEG49 N. A. N. A. Investigative [45]
Fenthion sulfoxide DM4OLRS N. A. N. A. Investigative [45]
flavone DMEQH6J Discovery agent N.A. Investigative [46]
Levoverbenone DMV3P89 N. A. N. A. Investigative [47]
Nicotinyl alcohol DMO7M2N N. A. N. A. Investigative [48]
Phenazone DMCE985 Discovery agent N.A. Investigative [49]
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⏷ Show the Full List of 7 Investigative Drug(s)
Molecule Interaction Atlas

References

1 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
2 Apremilast (Otezla): a new oral treatment for adults with psoriasis and psoriatic arthritis. P T. 2015 Aug;40(8):495-500.
3 A comparison of the expression and metabolizing activities of phase I and II enzymes in freshly isolated human lung parenchymal cells and cryopreserved human hepatocytes. Drug Metab Dispos. 2007 Oct;35(10):1797-805.
4 Identification of the human cytochrome P450 enzymes involved in the in vitro metabolism of artemisinin. Br J Clin Pharmacol. 1999 Oct;48(4):528-35.
5 Identification of human cytochrome P(450)s that metabolise anti-parasitic drugs and predictions of in vivo drug hepatic clearance from in vitro data. Eur J Clin Pharmacol. 2003 Sep;59(5-6):429-42.
6 Azelastine N-demethylation by cytochrome P-450 (CYP)3A4, CYP2D6, and CYP1A2 in human liver microsomes: evaluation of approach to predict the contribution of multiple CYPs. Drug Metab Dispos. 1999 Dec;27(12):1381-91.
7 In vitro metabolism of (-)-camphor using human liver microsomes and CYP2A6. Biol Pharm Bull. 2007 Feb;30(2):230-3.
8 FDA label of Cenobamate. The 2020 official website of the U.S. Food and Drug Administration.
9 Prediction of human liver microsomal oxidations of 7-ethoxycoumarin and chlorzoxazone with kinetic parameters of recombinant cytochrome P-450 enzymes. Drug Metab Dispos. 1999 Nov;27(11):1274-80.
10 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
11 Identification of the cytochrome P450 enzymes involved in the metabolism of cisapride: in vitro studies of potential co-medication interactions. Br J Pharmacol. 2000 Apr;129(8):1655-67.
12 Oxidative metabolism of flunarizine and cinnarizine by microsomes from B-lymphoblastoid cell lines expressing human cytochrome P450 enzymes. Biol Pharm Bull. 1996 Nov;19(11):1511-4.
13 Characterization of human cytochrome P450s involved in the bioactivation of clozapine. Drug Metab Dispos. 2013 Mar;41(3):651-8.
14 Development of a substrate-activity based approach to identify the major human liver P-450 catalysts of cyclophosphamide and ifosfamide activation based on cDNA-expressed activities and liver microsomal P-450 profiles. Drug Metab Dispos. 1999 Jun;27(6):655-66.
15 Clinical pharmacokinetics and pharmacodynamics of dapagliflozin, a selective inhibitor of sodium-glucose co-transporter type 2. Clin Pharmacokinet. 2014 Jan;53(1):17-27.
16 Impact of CYP2A6 gene polymorphism on the pharmacokinetics of dexmedetomidine for premedication. Expert Rev Clin Pharmacol. 2018 Sep;11(9):917-922.
17 CYP3A4 is the major CYP isoform mediating the in vitro hydroxylation and demethylation of flunitrazepam. Drug Metab Dispos. 2001 Feb;29(2):133-40.
18 Roles of cytochromes P450 1A2, 2A6, and 2C8 in 5-fluorouracil formation from tegafur, an anticancer prodrug, in human liver microsomes. Drug Metab Dispos. 2000 Dec;28(12):1457-63.
19 Is 1-aminobenzotriazole an appropriate in vitro tool as a nonspecific cytochrome P450 inactivator? Drug Metab Dispos. 2009 Jan;37(1):10-3.
20 Halothane-dependent lipid peroxidation in human liver microsomes is catalyzed by cytochrome P4502A6 (CYP2A6). Anesthesiology. 2001 Aug;95(2):509-14.
21 Measurement of 4-hydroxylation of ifosfamide in human liver microsomes using the estimation of free and protein-bound acrolein and codetermination of keto- and carboxyifosfamide. J Cancer Res Clin Oncol. 2002 Jul;128(7):385-92.
22 Letrozole concentration is associated with CYP2A6 variation but not with arthralgia in patients with breast cancer. Breast Cancer Res Treat. 2018 Nov;172(2):371-379.
23 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
24 Identification of human cytochrome P450 and flavin-containing monooxygenase enzymes involved in the metabolism of lorcaserin, a novel selective human 5-hydroxytryptamine 2C agonist. Drug Metab Dispos. 2012 Apr;40(4):761-71.
25 Health control over the feeding of troops on the Western and 3d Belorussian Fronts during the Great Patriotic War years. Voen Med Zh. 1975 Jun;(6):86-8.
26 Human kidney methoxyflurane and sevoflurane metabolism. Intrarenal fluoride production as a possible mechanism of methoxyflurane nephrotoxicity. Anesthesiology. 1995 Mar;82(3):689-99.
27 The role of human cytochrome P450 enzymes in the formation of 2-hydroxymetronidazole: CYP2A6 is the high affinity (low Km) catalyst. Drug Metab Dispos. 2013 Sep;41(9):1686-94.
28 CYP2A6- and CYP2A13-catalyzed metabolism of the nicotine delta-5'(1')iminium ion. J Pharmacol Exp Ther. 2012 Nov;343(2):307-15.
29 Identification of the human cytochrome P450 enzymes involved in the in vitro biotransformation of lynestrenol and norethindrone. J Steroid Biochem Mol Biol. 2008 May;110(1-2):56-66.
30 The metabolism of the piperazine-type phenothiazine neuroleptic perazine by the human cytochrome P-450 isoenzymes. Eur Neuropsychopharmacol. 2004 May;14(3):199-208.
31 Structural comparison of cytochromes P450 2A6, 2A13, and 2E1 with pilocarpine. FEBS J. 2012 May;279(9):1621-31.
32 Possible involvement of multiple human cytochrome P450 isoforms in the liver metabolism of propofol. Br J Anaesth. 1998 Jun;80(6):788-95.
33 Variation in CYP2A6 activity and personalized medicine. J Pers Med. 2017 Dec 1;7(4). pii: E18.
34 Genotoxicity of tamoxifen, tamoxifen epoxide and toremifene in human lymphoblastoid cells containing human cytochrome P450s. Carcinogenesis. 1994 Jan;15(1):5-9.
35 Rapid development of S-1 in the west for therapy of advanced gastric carcinoma. Gan To Kagaku Ryoho. 2006 Jun;33 Suppl 1:117-20.
36 Metabolism of thalidomide in human microsomes, cloned human cytochrome P-450 isozymes, and Hansen's disease patients. J Biochem Mol Toxicol. 2000;14(3):140-7.
37 UFT Capsules (uracil-tegafur).
38 Psychotropic drug interactions with valproate. Clin Neuropharmacol. 2005 Mar-Apr;28(2):96-101.
39 Identification of the cytochrome P450 and other enzymes involved in the in vitro oxidative metabolism of a novel antidepressant, Lu AA21004. Drug Metab Dispos. 2012 Jul;40(7):1357-65.
40 Cytochrome P450 CYP1B1 interacts with 8-methoxypsoralen (8-MOP) and influences psoralen-ultraviolet A (PUVA) sensitivity. PLoS One. 2013 Sep 23;8(9):e75494.
41 In vitro characterization of the human biotransformation pathways of aplidine, a novel marine anti-cancer drug. Invest New Drugs. 2007 Feb;25(1):9-19.
42 Australian Public Assessment Report for asunaprevir.
43 Cytochrome P450 enzymes involved in the metabolic pathway of the histamine 2 (H2)-receptor antagonist roxatidine acetate by human liver microsomes. Arzneimittelforschung. 2001;51(8):651-8.
44 Activation of phenacetin O-deethylase activity by alpha-naphthoflavone in human liver microsomes. Xenobiotica. 1999 Sep;29(9):885-98.
45 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.
46 Site-specific oxidation of flavanone and flavone by cytochrome P450 2A6 in human liver microsomes. Xenobiotica. 2019 Jul;49(7):791-802.
47 Roles of human CYP2A6 and 2B6 and rat CYP2C11 and 2B1 in the 10-hydroxylation of (-)-verbenone by liver microsomes. Drug Metab Dispos. 2003 Aug;31(8):1049-53.
48 Stability of the nicotine metabolite ratio in ad libitum and reducing smokers. Cancer Epidemiol Biomarkers Prev. 2008 Jun;17(6):1396-400.
49 Identification of the human hepatic cytochromes P450 involved in the in vitro oxidation of antipyrine. Drug Metab Dispos. 1996 Apr;24(4):487-94.