General Information of Drug (ID: DMEBOFW)

Drug Name
Clofazimine Drug Info
Synonyms
clofazimine; 2030-63-9; Lamprene; Lampren; Chlofazimine; Clofazimina; Clofaziminum; Clofaziminum [INN-Latin]; B 663 (Pharmaceutical); Clofazimina [INN-Spanish]; B-663; NSC-141046; G 30320; UNII-D959AE5USF; B 663 (VAN); C27H22Cl2N4; 3-(p-Chloranilino)-10-(p-chlorphenyl)-2,10-dihydro-2-(isopropylimino)-phenazin; B 663; 3-(p-Chloroanilino)-10-(p-chlorophenyl)-2,10-dihydro-2-(isopropylimino)phenazine; 3-(p-Chloranilino)-10-(p-chlorophenyl)-2,10-dihydro-2-(isopropylimino)-phenazine; EINECS 217-980-2; CFZ; SMP2_000339; B 663, pharmaceutical; G-30320; Lamprene (TN); Liposome-encapsulated clofazimine; Clofazimine [USAN:INN:BAN]; G-30,320; Clofazimine (JAN/USP/INN); N,5-bis(4-chlorophenyl)-3-propan-2-yliminophenazin-2-amine; N,5-Bis(4-chlorophenyl)-3,5-dihydro-3-(isopropylimino)phenazin-2-amine; N,5-Bis(4-chlorophenyl)-3,5-dihydro-3-(1-methylethyl)imino)-2-phenazinamine; N,5-Bis(4-chlorophenyl)-3,5-dihydro-3-[(1-methylethyl)imino]-2-phenazinamine; N,5-bis(4-chlorophenyl)-3-(propan-2-ylimino)-3,5-dihydrophenazin-2-amine; (3Z)-N,5-bis(4-chlorophenyl)-3-[(1-methylethyl)imino]-3,5-dihydrophenazin-2-amine; 3-(p-Chloranilino)-10-(p-chlorophenyl)-2,10-dihydro-2-(isopropylimino)phenazine; 3-(p-Chloranilino)-10-(p-chlorphenyl)-2,10-dihydro-2-(isopropylimino)-phenazin [German]; Riminophenazine
Indication
Disease Entry ICD 11 Status REF
Crohn disease DD70 Approved [1]
Leprosy Approved [2]
Multibacillary leprosy Approved [2]
Pyoderma gangrenosum EB21 Approved [2]
Mycobacterium infection 1B10-1B21 Investigative [3]
Therapeutic Class
Antiinflammatory Agents
Cross-matching ID
PubChem CID
2794
ChEBI ID
CHEBI:3749
CAS Number
CAS 2030-63-9
TTD Drug ID
DMEBOFW
VARIDT Drug ID
DR00669
INTEDE Drug ID
DR0346
ACDINA Drug ID
D00956

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metronidazole DMTIVEN Abscess Approved [9]
Nitrofurantoin DM7PQIK Urinary tract infection GC08 Approved [10]
Hydroxystilbamidine Isethionate DMR5QS6 Blastomycosis 1F22 Approved [11]
Furazolidone DM3P6V7 Diarrhea ME05.1 Approved [12]
Proflavine DMF1X5P Sepsis 1G40-1G41 Approved [13]
MGB-BP-3 DMPBTVK Clostridium infection 1A04 Phase 2 [14]
⏷ Show the Full List of 6 Drug(s)
Drug(s) Transported By P-glycoprotein 1 (ABCB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Amoxicillin DMUYNEI Acute otitis media AB00 Approved [15]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [16]
Methotrexate DM2TEOL Anterior urethra cancer Approved [17]
Folic Acid DMEMBJC Colorectal carcinoma Approved [18]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [17]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [17]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [19]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [17]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [20]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [21]
⏷ Show the Full List of 10 Drug(s)
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 [22]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [23]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [24]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [25]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [26]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [27]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [28]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [29]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [23]
Verapamil DMA7PEW Angina pectoris BA40 Approved [30]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Bile salt export pump (ABCB11)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Glimepiride DM5FSJA Diabetic complication 5A2Y Approved [7]
Ezetimibe DM7A8TW Atherosclerosis BD40 Approved [31]
Glipizide DMZA5PQ Diabetic complication 5A2Y Approved [31]
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [32]
Indinavir DM0T3YH Human immunodeficiency virus infection 1C62 Approved [7]
Ofloxacin DM0VQN3 Acute gonococcal cervicitis Approved [31]
Primidone DM0WX6I Epilepsy 8A60-8A68 Approved [33]
Gefitinib DM15F0X Colon adenocarcinoma Approved [7]
Drospirenone DM1A9W3 Acne vulgaris ED80 Approved [34]
Nitrendipine DM21C09 Hypertension BA00-BA04 Approved [7]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metoclopramide DMFA5MY Nausea MD90 Approved [35]
Quinidine DMLPICK N. A. N. A. Approved [36]
Verapamil DMA7PEW Angina pectoris BA40 Approved [37]
Erythromycin DM4K7GQ Acne vulgaris ED80 Approved [38]
Clarithromycin DM4M1SG Acute maxillary sinusitis Approved [38]
Disopyramide DM5SYZP Long QT syndrome BC65.0 Approved [39]
Propranolol DM79NTF Angina pectoris BA40 Approved [40]
Amiodarone DMUTEX3 Tachyarrhythmias BC71 Approved [41]
Dofetilide DMPN1TW Sinus rhythm disorder BC9Y Approved [42]
Flecainide DMSQDLE Tachyarrhythmias BC71 Approved [38]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Bacterial Deoxyribonucleic acid (Bact DNA) TTS1W4A NOUNIPROTAC Modulator [4]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [5]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) Main DME DE4LYSA CP3A4_HUMAN Substrate [6]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Bile salt export pump (ABCB11) OTRU7THO ABCBB_HUMAN Gene/Protein Processing [7]
Potassium voltage-gated channel subfamily H member 2 (KCNH2) OTZX881H KCNH2_HUMAN Gene/Protein Processing [8]

References

1 FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 019500.
2 Clofazimine FDA Label
3 The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.
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5 Efflux pump inhibitors: targeting mycobacterial efflux systems to enhance TB therapy. J Antimicrob Chemother. 2016 Jan;71(1):17-26.
6 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
7 Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development. Toxicol Sci. 2010 Dec; 118(2):485-500.
8 Why are most phospholipidosis inducers also hERG blockers?. Arch Toxicol. 2017 Dec;91(12):3885-3895. doi: 10.1007/s00204-017-1995-9. Epub 2017 May 27.
9 DNA breakage due to metronidazole treatment. Mutat Res. 2001 Jul 1;478(1-2):153-8.
10 On the nature of the adaptive response induced by mitomycin C in Vibrio cholerae OGAWA 154 cells. Biochem Biophys Res Commun. 1996 Mar 27;220(3):509-14.
11 Interaction between hydroxystilbamidine and DNA. I. Binding isotherms and thermodynamics of the association. Biochim Biophys Acta. 1975 Sep 12;407(1):24-42.
12 Interaction of furazolidone with DNA. Biochim Biophys Acta. 1975 Aug 21;402(2):161-5.
13 Interaction of small molecules with double-stranded RNA: spectroscopic, viscometric, and calorimetric study of hoechst and proflavine binding to PolyCG structures. DNA Cell Biol. 2009 Apr;28(4):209-19.
14 Clinical pipeline report, company report or official report of MGB Biopharma.
15 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
16 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
17 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
18 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
19 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
20 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
21 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
22 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.
23 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
24 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.
25 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
26 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.
27 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.
28 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
29 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.
30 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.
31 Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43.
32 Omics-based responses induced by bosentan in human hepatoma HepaRG cell cultures. Arch Toxicol. 2018 Jun;92(6):1939-1952.
33 Evaluating the Role of Multidrug Resistance Protein 3 (MDR3) Inhibition in Predicting Drug-Induced Liver Injury Using 125 Pharmaceuticals. Chem Res Toxicol. 2017 May 15;30(5):1219-1229. doi: 10.1021/acs.chemrestox.7b00048. Epub 2017 May 4.
34 A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. Toxicol Sci. 2013 Nov;136(1):216-41.
35 Comparison of the effects of metoclopramide and domperidone on HERG channels. Pharmacology. 2005 Apr;74(1):31-6. doi: 10.1159/000083234. Epub 2005 Jan 7.
36 Further insights into the effect of quinidine in short QT syndrome caused by a mutation in HERG. J Cardiovasc Electrophysiol. 2005 Jan;16(1):54-8. doi: 10.1046/j.1540-8167.2005.04470.x.
37 Automated tight seal electrophysiology for assessing the potential hERG liability of pharmaceutical compounds. Assay Drug Dev Technol. 2004 Oct;2(5):497-506. doi: 10.1089/adt.2004.2.497.
38 Refining the human iPSC-cardiomyocyte arrhythmic risk assessment model. Toxicol Sci. 2013 Dec;136(2):581-94. doi: 10.1093/toxsci/kft205. Epub 2013 Sep 19.
39 Pharmacology of the short QT syndrome N588K-hERG K+ channel mutation: differential impact on selected class I and class III antiarrhythmic drugs. Br J Pharmacol. 2008 Nov;155(6):957-66. doi: 10.1038/bjp.2008.325. Epub 2008 Aug 25.
40 Comparison of HERG channel blocking effects of various beta-blockers-- implication for clinical strategy. Br J Pharmacol. 2006 Mar;147(6):642-52. doi: 10.1038/sj.bjp.0706508.
41 Inhibitory effects of the class III antiarrhythmic drug amiodarone on cloned HERG potassium channels. Naunyn Schmiedebergs Arch Pharmacol. 1999 Mar;359(3):212-9. doi: 10.1007/pl00005344.
42 Redox state dependency of HERGS631C channel pharmacology: relation to C-type inactivation. FEBS Lett. 2000 May 26;474(1):111-5. doi: 10.1016/s0014-5793(00)01586-6.