Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMOYE70)

Drug Name
Fexinidazole Drug Info
Synonyms
Fexinidazole (human African trypanosomiasis); Fexinidazole (African sleeping sickness), Drugs for Neglected Diseases initiative; Fexinidazole (HAT), Drugs for Neglected Diseases initiative; Fexinidazole (human African trypanosomiasis), Drugs for Neglected Diseases initiative
Indication
Disease Entry ICD 11 Status REF
African trypanosomiasis 1F51 Approved [1]
Trypanosomiasis 1D51-1F53 Phase 2/3 [2]
Cross-matching ID
PubChem CID
68792
CAS Number
CAS 59729-37-2
TTD Drug ID
DMOYE70
INTEDE Drug ID
DR1873

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DME
Drug Status:
Approved Drug(s)
Download the Complete Related Drug List
Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [4]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [5]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [6]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [7]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [8]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [9]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [10]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [11]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [5]
Verapamil DMA7PEW Angina pectoris BA40 Approved [12]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 1A2 (CYP1A2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [13]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [14]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [15]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [16]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [17]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [18]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [10]
Oxaliplatin DMQNWRD Adenocarcinoma 2D40 Approved [19]
Verapamil DMA7PEW Angina pectoris BA40 Approved [20]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [21]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 2D6 (CYP2D6)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [22]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [23]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [24]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [8]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [12]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [25]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [26]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [27]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [28]
Propranolol DM79NTF Angina pectoris BA40 Approved [29]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 3A5 (CYP3A5)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [30]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [31]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [32]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [33]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [34]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [35]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [36]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [37]
Verapamil DMA7PEW Angina pectoris BA40 Approved [38]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [33]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 2B6 (CYP2B6)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [39]
Verapamil DMA7PEW Angina pectoris BA40 Approved [40]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [41]
Estrone DM5T6US Acne vulgaris ED80 Approved [42]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [43]
Irinotecan DMP6SC2 Adenocarcinoma 2D40 Approved [44]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [45]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [46]
Phenytoin DMNOKBV Epilepsy 8A60-8A68 Approved [47]
Amitriptyline DMK7F9S Depression 6A70-6A7Z Approved [48]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Mephenytoin 4-hydroxylase (CYP2C19)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Amoxicillin DMUYNEI Acute otitis media AB00 Approved [49]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [50]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [51]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [52]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [40]
Verapamil DMA7PEW Angina pectoris BA40 Approved [53]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [54]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [55]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [56]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [57]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas
Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [3]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Substrate [3]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Substrate [3]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Substrate [3]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [3]
Cytochrome P450 2B6 (CYP2B6) DEPKLMQ CP2B6_HUMAN Substrate [3]

References

1 FDA Approved Drug Products from FDA Official Website. 2021. Application Number: 214429.
2 ClinicalTrials.gov (NCT02169557) Efficacy and Safety of Fexinidazole in Patients With Stage 1 or Early Stage 2 Human African Trypanosomiasis (HAT) Due to T.b. Gambiense: a Prospective, Multicentre, Open-label Cohort Study, plug-in to the Pivotal Study. U.S. National Institutes of Health.
3 Fexinidazole--a new oral nitroimidazole drug candidate entering clinical development for the treatment of sleeping sickness. PLoS Negl Trop Dis. 2010 Dec 21;4(12):e923.
4 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
5 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
6 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
7 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
8 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.
9 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
10 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
11 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
12 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.
13 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.
14 Effects of polyunsaturated fatty acids on prostaglandin synthesis and cyclooxygenase-mediated DNA adduct formation by heterocyclic aromatic amines in human adenocarcinoma colon cells. Mol Carcinog. 2004 Jul;40(3):180-8.
15 Endoxifen and other metabolites of tamoxifen inhibit human hydroxysteroid sulfotransferase 2A1 (hSULT2A1). Drug Metab Dispos. 2014 Nov;42(11):1843-50.
16 Cytochrome P450 1A2 (CYP1A2) activity and risk factors for breast cancer: a cross-sectional study. Breast Cancer Res. 2004;6(4):R352-65.
17 PharmGKB summary: pathways of acetaminophen metabolism at the therapeutic versus toxic doses. Pharmacogenet Genomics. 2015 Aug;25(8):416-26.
18 The effect of apigenin on pharmacokinetics of imatinib and its metabolite N-desmethyl imatinib in rats. Biomed Res Int. 2013;2013:789184.
19 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.
20 Identification of P450 enzymes involved in metabolism of verapamil in humans. Naunyn Schmiedebergs Arch Pharmacol. 1993 Sep;348(3):332-7.
21 Metabolism and metabolic inhibition of xanthotoxol in human liver microsomes. Evid Based Complement Alternat Med. 2016;2016:5416509.
22 Inhibitory effects of anticancer drugs on dextromethorphan-O-demethylase activity in human liver microsomes. Cancer Chemother Pharmacol. 1993;32(6):491-5.
23 Effect of genetic polymorphism on the metabolism of endogenous neuroactive substances, progesterone and p-tyramine, catalyzed by CYP2D6. Brain Res Mol Brain Res. 2004 Oct 22;129(1-2):117-23.
24 CYP2D6 polymorphisms and tamoxifen metabolism: clinical relevance. Curr Oncol Rep. 2010 Jan;12(1):7-15.
25 Inhibition of cytochrome P450 2D6: structure-activity studies using a series of quinidine and quinine analogues. Chem Res Toxicol. 2003 Apr;16(4):450-9.
26 Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53.
27 Pharmacogenetics of schizophrenia. Am J Med Genet. 2000 Spring;97(1):98-106.
28 Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70.
29 Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82.
30 Drug related genetic polymorphisms affecting adverse reactions to methotrexate, vinblastine, doxorubicin and cisplatin in patients with urothelial cancer. J Urol. 2008 Dec;180(6):2389-95.
31 Human prostate CYP3A5: identification of a unique 5'-untranslated sequence and characterization of purified recombinant protein. Biochem Biophys Res Commun. 1999 Jul 14;260(3):676-81.
32 Polymorphisms in cytochrome P4503A5 (CYP3A5) may be associated with race and tumor characteristics, but not metabolism and side effects of tamoxifen in breast cancer patients. Cancer Lett. 2005 Jan 10;217(1):61-72.
33 Drug Interactions Flockhart Table
34 Induction of hepatic CYP2E1 by a subtoxic dose of acetaminophen in rats: increase in dichloromethane metabolism and carboxyhemoglobin elevation. Drug Metab Dispos. 2007 Oct;35(10):1754-8.
35 Urinary 6 beta-hydroxycortisol excretion in rheumatoid arthritis. Br J Rheumatol. 1997 Jan;36(1):54-8.
36 Clinical pharmacokinetics of imatinib. Clin Pharmacokinet. 2005;44(9):879-94.
37 Kinetics and regulation of cytochrome P450-mediated etoposide metabolism. Drug Metab Dispos. 2004 Sep;32(9):993-1000.
38 Differential mechanism-based inhibition of CYP3A4 and CYP3A5 by verapamil. Drug Metab Dispos. 2005 May;33(5):664-71.
39 Effect of tamoxifen on the enzymatic activity of human cytochrome CYP2B6. J Pharmacol Exp Ther. 2002 Jun;301(3):945-52.
40 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
41 Hepatic metabolism of diclofenac: role of human CYP in the minor oxidative pathways. Biochem Pharmacol. 1999 Sep 1;58(5):787-96.
42 Characterization of the oxidative metabolites of 17beta-estradiol and estrone formed by 15 selectively expressed human cytochrome p450 isoforms. Endocrinology. 2003 Aug;144(8):3382-98.
43 Insights into CYP2B6-mediated drug-drug interactions. Acta Pharm Sin B. 2016 Sep;6(5):413-425.
44 Drugs that may have potential CYP2B6 interactions.
45 Involvement of human cytochrome P450 2B6 in the omega- and 4-hydroxylation of the anesthetic agent propofol. Xenobiotica. 2007 Jul;37(7):717-24.
46 Nicotine and 4-(methylnitrosamino)-1-(3-pyridyl)-butanone metabolism by cytochrome P450 2B6. Drug Metab Dispos. 2005 Dec;33(12):1760-4.
47 PharmGKB summary: phenytoin pathway. Pharmacogenet Genomics. 2012 Jun;22(6):466-70.
48 Application of the relative activity factor approach in scaling from heterologously expressed cytochromes p450 to human liver microsomes: studies on amitriptyline as a model substrate. J Pharmacol Exp Ther. 2001 Apr;297(1):326-37.
49 High-dose rabeprazole/amoxicillin therapy as the second-line regimen after failure to eradicate H. pylori by triple therapy with the usual doses of a proton pump inhibitor, clarithromycin and amoxicillin. Hepatogastroenterology. 2003 Nov-Dec;50(54):2274-8.
50 Progesterone and testosterone hydroxylation by cytochromes P450 2C19, 2C9, and 3A4 in human liver microsomes. Arch Biochem Biophys. 1997 Oct 1;346(1):161-9.
51 Cytochrome P450 pharmacogenetics and cancer. Oncogene. 2006 Mar 13;25(11):1679-91.
52 CYP2C19*17 is associated with decreased breast cancer risk. Breast Cancer Res Treat. 2009 May;115(2):391-6.
53 Cytochromes of the P450 2C subfamily are the major enzymes involved in the O-demethylation of verapamil in humans. Naunyn Schmiedebergs Arch Pharmacol. 1995 Dec;353(1):116-21.
54 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.
55 A mechanistic approach to antiepileptic drug interactions. Ann Pharmacother. 1998 May;32(5):554-63.
56 Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33.
57 Possible involvement of multiple human cytochrome P450 isoforms in the liver metabolism of propofol. Br J Anaesth. 1998 Jun;80(6):788-95.