General Information of DME (ID: DE6OQ3W)

DME Name Cytochrome P450 1A1 (CYP1A1) DME Info
Gene Name CYP1A1

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Discontinued Drug(s)
Approved Drug(s)
Clinical Trial Drug(s)
Investigative Drug(s)
44 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]
Amiodarone DMUTEX3 Tachyarrhythmias BC71 Approved [2]
Amodiaquine DME4RA8 Malaria 1F40-1F45 Approved [3]
BAY 80-6946 DMLOS5R Follicular lymphoma 2A80 Approved [4]
Capsaicin DMGMF6V Back pain ME84.Z Approved [5]
Chloroquine DMSI5CB Malaria 1F40-1F45 Approved [6]
Clenbuterol DMCKYZ5 Chronic breathing disorder 7A4Z Approved [7]
Clofibrate DMPC1J7 Dysbetalipoproteinemia 5C80.2 Approved [8]
Dacarbazine DMNPZL4 Adenocarcinoma 2D40 Approved [9]
Daunorubicin DMQUSBT Acute monocytic leukemia Approved [10]
Debrisoquin DMC50ME Hypertension BA00-BA04 Approved [11]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [12]
Erythromycin DM4K7GQ Acne vulgaris ED80 Approved [13]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [14]
Estrone DM5T6US Acne vulgaris ED80 Approved [15]
Ethacrynic acid DM60QMR Edema MG29 Approved [16]
Ethinyl Estradiol DMODJ40 Acne vulgaris ED80 Approved [17]
Flunarizine DMZU5JP Migraine 8A80 Approved [8]
Flutamide DMK0O7U Prostate cancer 2C82.0 Approved [18]
Fluvastatin DM4MDJY Arteriosclerosis BD40 Approved [19]
Granisetron DMIUW25 Malignant glioma 2A00.0 Approved [20]
Haloperidol DM96SE0 Delirium Approved [21]
Ipriflavone DM0IO13 Osteoporosis FB83.0 Approved [22]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [23]
Melatonin DMKWFBT Depression 6A70-6A7Z Approved [24]
Menadione DMSJDTY Vitamin K deficiency 5B59 Approved [25]
Mercaptopurine DMTM2IK Acute lymphoblastic leukaemia 2A85 Approved [26]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [27]
Oxaliplatin DMQNWRD Adenocarcinoma 2D40 Approved [28]
Perazine DM2AOTZ Psychotic disorder 6A20-6A25 Approved [29]
Prazosin DMCD9YG Benign prostatic hyperplasia GA90 Approved [30]
Procarbazine DMIK367 Hodgkin lymphoma 2B30 Approved [31]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [32]
Raltegravir DMYURI6 Human immunodeficiency virus infection 1C62 Approved [33]
Retigabine DMGNYIH Behcet disease 4A62 Approved [34]
Riboflavin DM8YMWE Acne vulgaris ED80 Approved [35]
Riluzole DMECBWN Amyotrophic lateral sclerosis 8B60.0 Approved [36]
Riociguat DMXBLMP Chronic thromboembolic pulmonary hypertension Approved [37]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [38]
Testosterone cypionate DMC1TEV N. A. N. A. Approved [32]
Theophylline DMRJFN9 Bronchitis CA20 Approved [39]
Toremifene DMQYUWG Breast cancer 2C60-2C65 Approved [40]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [41]
ZOTEPINE DMF3VXA Anxiety disorder 6B00-6B0Z Approved [42]
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⏷ Show the Full List of 44 Approved Drug(s)
7 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 [43]
MK-4827 DMLYGH4 Ovarian cancer 2C73 Phase 3 [44]
AFQ056 DMMHSLC Fragile X syndrome LD55 Phase 2/3 [45]
2-Methoxyestradiol DMGBPME Pulmonary arterial hypertension BB01.0 Phase 2 [46]
9-AMINOCAMPTOTHECIN DMQXYRG Acquired immune deficiency syndrome 1C62.3 Phase 2 [47]
Famitinib DMSFWT7 Solid tumour/cancer 2A00-2F9Z Phase 2 [48]
SALVINORIN A DMJ3HQY Cerebral vasospasm BA85.Z Phase 1 [49]
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⏷ Show the Full List of 7 Clinical Trial Drug(s)
2 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 [50]
Benzydamine DMEQL9U Chemotherapy or radiotherapy-induced mucositis DA42-DA60 Discontinued in Phase 2 [51]
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1 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Acriflavinium chloride DMYZJ5B N. A. N. A. Investigative [52]
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Molecule Interaction Atlas

References

1 Preferred orientations in the binding of 4'-hydroxyacetanilide (acetaminophen) to cytochrome P450 1A1 and 2B1 isoforms as determined by 13C- and 15N-NMR relaxation studies. J Med Chem. 1994 Mar 18;37(6):860-7.
2 A significant role of human cytochrome P450 2C8 in amiodarone N-deethylation: an approach to predict the contribution with relative activity factor. Drug Metab Dispos. 2000 Nov;28(11):1303-10.
3 Amodiaquine clearance and its metabolism to N-desethylamodiaquine is mediated by CYP2C8: a new high affinity and turnover enzyme-specific probe substrate. J Pharmacol Exp Ther. 2002 Feb;300(2):399-407.
4 FDA label of Copanlisib. The 2020 official website of the U.S. Food and Drug Administration.
5 Metabolism of capsaicin by cytochrome P450 produces novel dehydrogenated metabolites and decreases cytotoxicity to lung and liver cells. Chem Res Toxicol. 2003 Mar;16(3):336-49.
6 In vitro metabolism of chloroquine: identification of CYP2C8, CYP3A4, and CYP2D6 as the main isoforms catalyzing N-desethylchloroquine formation. Drug Metab Dispos. 2003 Jun;31(6):748-54.
7 Beta-adrenergic receptor modulation of the LPS-mediated depression in CYP1A activity in astrocytes. Biochem Pharmacol. 2005 Mar 1;69(5):741-50.
8 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.
9 Metabolic activation of dacarbazine by human cytochromes P450: the role of CYP1A1, CYP1A2, and CYP2E1. Clin Cancer Res. 1999 Aug;5(8):2192-7.
10 The effect of new lipophilic chelators on the activities of cytosolic reductases and P450 cytochromes involved in the metabolism of anthracycline antibiotics: studies in vitro. Physiol Res. 2004;53(6):683-91.
11 4-Hydroxylation of debrisoquine by human CYP1A1 and its inhibition by quinidine and quinine. J Pharmacol Exp Ther. 2002 Jun;301(3):1025-32.
12 Diclofenac and its derivatives as tools for studying human cytochromes P450 active sites: particular efficiency and regioselectivity of P450 2Cs. Biochemistry. 1999 Oct 26;38(43):14264-70.
13 Cytochromes P450 in crustacea. Comp Biochem Physiol C Pharmacol Toxicol Endocrinol. 1998 Nov;121(1-3):157-72.
14 Cytochrome P450 isoforms catalyze formation of catechol estrogen quinones that react with DNA. Metabolism. 2007 Jul;56(7):887-94.
15 A common CYP1B1 polymorphism is associated with 2-OHE1/16-OHE1 urinary estrone ratio. Clin Chem Lab Med. 2005;43(7):702-6.
16 Xenobiotic metabolizing and antioxidant enzymes in normal and neoplastic human breast tissue. Eur J Drug Metab Pharmacokinet. 1998 Oct-Dec;23(4):497-500.
17 The involvement of CYP3A4 and CYP2C9 in the metabolism of 17 alpha-ethinylestradiol. Drug Metab Dispos. 2004 Nov;32(11):1209-12.
18 Human CYP1B1 and anticancer agent metabolism: mechanism for tumor-specific drug inactivation? J Pharmacol Exp Ther. 2001 Feb;296(2):537-41.
19 Regulation of cytochrome P450 expression by inhibitors of hydroxymethylglutaryl-coenzyme A reductase in primary cultured rat hepatocytes and in rat liver. Drug Metab Dispos. 1996 Nov;24(11):1197-204.
20 CYP1A1 is a major enzyme responsible for the metabolism of granisetron in human liver microsomes. Curr Drug Metab. 2005 Oct;6(5):469-80.
21 In vitro characterization of the metabolism of haloperidol using recombinant cytochrome p450 enzymes and human liver microsomes. Drug Metab Dispos. 2001 Dec;29(12):1638-43.
22 Effects of enzyme inducers and inhibitors on the pharmacokinetics of intravenous ipriflavone in rats. J Pharm Pharmacol. 2006 Apr;58(4):449-57.
23 Increasing the intracellular availability of all-trans retinoic acid in neuroblastoma cells. Br J Cancer. 2005 Feb 28;92(4):696-704.
24 Metabolism of melatonin by human cytochromes p450. Drug Metab Dispos. 2005 Apr;33(4):489-94.
25 Rat hepatic CYP1A1 and CYP1A2 induction by menadione. Toxicol Lett. 2005 Feb 15;155(2):253-8.
26 Pharmacogenomics in drug-metabolizing enzymes catalyzing anticancer drugs for personalized cancer chemotherapy. Curr Drug Metab. 2007 Aug;8(6):554-62.
27 Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70.
28 The influence of metabolic gene polymorphisms on urinary 1-hydroxypyrene concentrations in Chinese coke oven workers. Sci Total Environ. 2007 Aug 1;381(1-3):38-46.
29 The metabolism of the piperazine-type phenothiazine neuroleptic perazine by the human cytochrome P-450 isoenzymes. Eur Neuropsychopharmacol. 2004 May;14(3):199-208.
30 Role of adrenoceptor-linked signaling pathways in the regulation of CYP1A1 gene expression. Biochem Pharmacol. 2005 Jan 15;69(2):277-87.
31 In vitro and in vivo evidence for the formation of methyl radical from procarbazine: a spin-trapping study. Carcinogenesis. 1992 May;13(5):799-805.
32 Allelic variants of human cytochrome P450 1A1 (CYP1A1): effect of T461N and I462V substitutions on steroid hydroxylase specificity. Pharmacogenetics. 2000 Aug;10(6):519-30.
33 Exposure-related effects of atazanavir on the pharmacokinetics of raltegravir in HIV-1-infected patients. Ther Drug Monit. 2010 Dec;32(6):782-6.
34 Retigabine N-glucuronidation and its potential role in enterohepatic circulation. Drug Metab Dispos. 1999 May;27(5):605-12.
35 Disruption of endogenous regulator homeostasis underlies the mechanism of rat CYP1A1 mRNA induction by metyrapone. Biochem J. 1998 Apr 1;331 ( Pt 1):273-81.
36 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
37 Riociguat (adempas): a novel agent for the treatment of pulmonary arterial hypertension and chronic thromboembolic pulmonary hypertension. P T. 2014 Nov;39(11):749-58.
38 Metabolism of tamoxifen by recombinant human cytochrome P450 enzymes: formation of the 4-hydroxy, 4'-hydroxy and N-desmethyl metabolites and isomerization of trans-4-hydroxytamoxifen. Drug Metab Dispos. 2002 Aug;30(8):869-74.
39 Specificity of substrate and inhibitor probes for human cytochromes P450 1A1 and 1A2. J Pharmacol Exp Ther. 1993 Apr;265(1):401-7.
40 Involvement of cytochrome P450 3A enzyme family in the major metabolic pathways of toremifene in human liver microsomes. Biochem Pharmacol. 1994 May 18;47(10):1883-95.
41 Oxidation of troglitazone to a quinone-type metabolite catalyzed by cytochrome P-450 2C8 and P-450 3A4 in human liver microsomes. Drug Metab Dispos. 1999 Nov;27(11):1260-6.
42 Identification of cytochrome P450 enzymes involved in the metabolism of zotepine, an antipsychotic drug, in human liver microsomes. Xenobiotica. 1999 Mar;29(3):217-29.
43 Cytochrome P450 CYP1B1 interacts with 8-methoxypsoralen (8-MOP) and influences psoralen-ultraviolet A (PUVA) sensitivity. PLoS One. 2013 Sep 23;8(9):e75494.
44 Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. J Med Chem. 2009 Nov 26;52(22):7170-85.
45 Methods to Assess Pulmonary Metabolism.
46 Role of 2-methoxyestradiol, an Endogenous Estrogen Metabolite, in Health and Disease. Mini Rev Med Chem. 2015;15(5):427-38.
47 Cytochrome P450 3A-mediated metabolism of the topoisomerase I inhibitor 9-aminocamptothecin: impact on cancer therapy. Int J Oncol. 2014 Aug;45(2):877-86.
48 Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
49 Evaluation of the transport, in vitro metabolism and pharmacokinetics of Salvinorin A, a potent hallucinogen. Eur J Pharm Biopharm. 2009 Jun;72(2):471-7.
50 Identification of CYP3A4 as the enzyme involved in the mono-N-dealkylation of disopyramide enantiomers in humans. Drug Metab Dispos. 2000 Aug;28(8):937-44.
51 In vitro evaluation of potential in vivo probes for human flavin-containing monooxygenase (FMO): metabolism of benzydamine and caffeine by FMO and P450 isoforms. Br J Clin Pharmacol. 2000 Oct;50(4):311-4.
52 Activation of the antitumor agent aminoflavone (NSC 686288) is mediated by induction of tumor cell cytochrome P450 1A1/1A2. Mol Pharmacol. 2002 Jul;62(1):143-53.