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

General Information of Drug (ID: DMGUZ0W)

Drug Name
MELARSOPROL Drug Info
Synonyms
MELARSOPROL; Mel B; Arsobal; 494-79-1; Melarsoprolum [INN-Latin]; EINECS 207-793-4; Melarsoprol [INN:BAN:DCF]; RP 3854; CHEBI:6729; [2-[4-[(4,6-diamino-1,3,5-triazin-2-yl)amino]phenyl]-1,3,2-dithiarsolan-4-yl]methanol; 1,3,2-Dithiarsolane-4-methanol, 2-(4-((4,6-diamino-1,3,5-triazin-2-yl)amino)phenyl)-; Melarsoprolum; Melarsenoxid-BAL; 2-(p-(4,6-Diamino-s-triazin-2-ylamino)phenyl)-1,3,2-dithiarsolane-4-methanol; C12H15AsN6OS2; Specia; UNII-ZF3786Q2E8; Melarsoprol (INN); AC1L1UXN; Mel B (TN); CHEMBL166; SCHEMBL61707; ZF3786Q2E8
Indication
Disease Entry ICD 11 Status REF
Trypanosomiasis 1D51-1F53 Approved [1]
Cross-matching ID
PubChem CID
10311
ChEBI ID
CHEBI:6729
CAS Number
CAS 494-79-1
TTD Drug ID
DMGUZ0W

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Investigative Drug(s)
Approved Drug(s)
Download the Complete Related Drug List
Drug(s) Targeting Cysteine protease (CYP)
Drug Name Drug ID Indication ICD 11 Highest Status REF
K-777 DMIFCMW Discovery agent N.A. Investigative [6]
N-methyl-Pip-F-homoF-vinyl sulfonyl phenyl (N-methyl-Pip-F-hF-VS phi) DMDAN0K Discovery agent N.A. Investigative [7]
S-hexyl hexane-1-sulfinothioate DMODS9A Discovery agent N.A. Investigative [8]
S-benzyl phenylmethanesulfinothioate DMDUC2X Discovery agent N.A. Investigative [8]
S-isopentyl 3-methylbutane-1-sulfinothioate DM1NXFL Discovery agent N.A. Investigative [8]
S-propyl propane-1-sulfinothioate DMFTLY9 Discovery agent N.A. Investigative [8]
ALLICIN DMSOJ6H Discovery agent N.A. Investigative [8]
⏷ Show the Full List of 7 Drug(s)
Drug(s) Affected By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Eplerenone DMF0NQR Heart failure BD10-BD13 Approved [9]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [10]
Isotretinoin DM4QTBN Acne vulgaris ED80 Approved [11]
Voriconazole DMAOL2S Aspergillosis 1F20 Approved [12]
Proguanil DMBL79I Malaria 1F40-1F45 Approved [5]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [5]
Loratadine DMF3AN7 Allergy 4A80-4A85 Approved [13]
Nelfinavir mesylate DMFX6G8 N. A. N. A. Approved [14]
Capsaicin DMGMF6V Back pain ME84.Z Approved [15]
Axitinib DMGVH6N Renal cell carcinoma 2C90 Approved [16]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Cytochrome P450 2D6 (CYP2D6)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [17]
Paliperidone DM7NPJS Psychotic disorder 6A20-6A25 Approved [18]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [19]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [20]
Oxatomide DM1F42Z Hay fever CA08.00 Approved [21]
Cinacalcet DMCX0K3 Hyperparathyroidism 5A51 Approved [22]
Capsaicin DMGMF6V Back pain ME84.Z Approved [23]
Pentamidine DMHZJCG African trypanosomiasis 1F51 Approved [5]
Quinidine DMLPICK N. A. N. A. Approved [24]
Buprenorphine DMPRI8G Opioid dependence 6C43.2Z Approved [25]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Cytochrome P450 2C9 (CYP2C9)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [10]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [26]
Dapsone DM4LT8A Acne vulgaris ED80 Approved [5]
Voriconazole DMAOL2S Aspergillosis 1F20 Approved [12]
Capsaicin DMGMF6V Back pain ME84.Z Approved [23]
Zafirlukast DMHNQOG Asthma CA23 Approved [27]
Niclosamide DMJAGXQ Cestodes infection 1F70-1F76 Approved [5]
Eicosapentaenoic acid/docosa-hexaenoic acid DMMUCG4 Hypertriglyceridemia 5C80.1 Approved [28]
Fluconazole DMOWZ6B Cryptococcal meningitis Approved [12]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [5]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Cytochrome P450 2C19 (CYP2C19)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [10]
Thioridazine DM35M8J Schizophrenia 6A20 Approved [29]
Voriconazole DMAOL2S Aspergillosis 1F20 Approved [12]
Chloramphenicol DMFXEWT Bacterial infection 1A00-1C4Z Approved [30]
Capsaicin DMGMF6V Back pain ME84.Z Approved [23]
Pentamidine DMHZJCG African trypanosomiasis 1F51 Approved [5]
Stiripentol DMMSDOY Dravet syndrome 8A61.11 Approved [31]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [5]
Desipramine DMT2FDC Attention deficit hyperactivity disorder 6A05.Z Approved [29]
Amitriptyline DMK7F9S Depression 6A70-6A7Z Approved [32]
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Drug(s) Affected By Poly polymerase 1 (PARP1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [33]
Gefitinib DM15F0X Colon adenocarcinoma Approved [34]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [35]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [36]
Citalopram DM2G9AE Acute coronary syndrome BA41 Approved [37]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [38]
Imipramine DM2NUH3 Depression 6A70-6A7Z Approved [37]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [39]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [40]
Methotrexate DM2TEOL Anterior urethra cancer Approved [41]
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Drug(s) Affected By Apoptosis regulator Bcl-2 (BCL2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sevoflurane DMC9O43 Anaesthesia 9A78.6 Approved [42]
Docetaxel DMDI269 Advanced cancer 2A00-2F9Z Approved [43]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [44]
Gemcitabine DMSE3I7 Anterior urethra cancer Approved [45]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [32]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [33]
Verapamil DMA7PEW Angina pectoris BA40 Approved [46]
Mechlorethamine DM0CVXA Chronic myelogenous leukaemia 2A20.0 Approved [47]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [48]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [49]
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Drug(s) Affected By Caspase-3 (CASP3)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sevoflurane DMC9O43 Anaesthesia 9A78.6 Approved [50]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [51]
Lovastatin DM9OZWQ Arteriosclerosis BD40 Approved [52]
Cidofovir DMA13GD Cytomegalovirus infection 1D82 Approved [53]
Docetaxel DMDI269 Advanced cancer 2A00-2F9Z Approved [54]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [55]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [56]
Mannitol DMSCDY9 Bronchiectasis CA24 Approved [57]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [58]
Aprepitant DM053KT Depression 6A70-6A7Z Approved [59]
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Molecular Interaction Atlas of This Drug

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

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Cysteine protease (CYP) TT2SUAQ NOUNIPROTAC Inhibitor [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Apoptosis regulator Bcl-2 (BCL2) OT9DVHC0 BCL2_HUMAN Gene/Protein Processing [3]
Caspase-3 (CASP3) OTIJRBE7 CASP3_HUMAN Gene/Protein Processing [4]
Cytochrome P450 2C19 (CYP2C19) OTFMJYYE CP2CJ_HUMAN Gene/Protein Processing [5]
Cytochrome P450 2C9 (CYP2C9) OTGLBN29 CP2C9_HUMAN Gene/Protein Processing [5]
Cytochrome P450 2D6 (CYP2D6) OTZJC802 CP2D6_HUMAN Gene/Protein Processing [5]
Cytochrome P450 3A4 (CYP3A4) OTQGYY83 CP3A4_HUMAN Gene/Protein Processing [5]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Protein Interaction/Cellular Processes [4]

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
2 On-bead screening of a combinatorial fumaric acid derived peptide library yields antiplasmodial cysteine protease inhibitors with unusual peptide s... J Med Chem. 2009 Sep 24;52(18):5662-72.
3 Comparative activity of melarsoprol and arsenic trioxide in chronic B-cell leukemia lines. Blood. 1997 Jul 15;90(2):562-70.
4 RIP kinase is involved in arsenic-induced apoptosis in multiple myeloma cells. Apoptosis. 2004 Sep;9(5):561-71. doi: 10.1023/B:APPT.0000038030.47068.49.
5 Application of higher throughput screening (HTS) inhibition assays to evaluate the interaction of antiparasitic drugs with cytochrome P450s. Drug Metab Dispos. 2001 Jan;29(1):30-5.
6 Novel non-peptidic vinylsulfones targeting the S2 and S3 subsites of parasite cysteine proteases. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6218-21.
7 A cysteine protease inhibitor cures Chagas' disease in an immunodeficient-mouse model of infection. Antimicrob Agents Chemother. 2007 Nov;51(11):3932-9.
8 Allicin and derivates are cysteine protease inhibitors with antiparasitic activity. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5541-3.
9 The relative role of CYP3A4 and CYP3A5 in eplerenone metabolism. Toxicol Lett. 2019 Oct 15;315:9-13.
10 Characterization of the structural determinants required for potent mechanism-based inhibition of human cytochrome P450 1A1 by cannabidiol. Chem Biol Interact. 2014 May 25;215:62-8.
11 Retinoids activate the RXR/SXR-mediated pathway and induce the endogenous CYP3A4 activity in Huh7 human hepatoma cells. Toxicol Sci. 2006 Jul;92(1):51-60.
12 The novel azole R126638 is a selective inhibitor of ergosterol synthesis in Candida albicans, Trichophyton spp., and Microsporum canis. Antimicrob Agents Chemother. 2004 Sep;48(9):3272-8.
13 Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity. Bioorg Med Chem Lett. 2004 Nov 15;14(22):5591-4.
14 Mechanism-based inactivation of CYP3A by HIV protease inhibitors. J Pharmacol Exp Ther. 2005 Feb;312(2):583-91.
15 Studies of the toxicological potential of capsinoids, XIII: inhibitory effects of capsaicin and capsinoids on cytochrome P450 3A4 in human liver microsomes. Int J Toxicol. 2010 Mar;29(2 Suppl):22S-6S.
16 Investigation of the effects of axitinib on the pharmacokinetics of loperamide and its main metabolite N-demethylated loperamide in rats by UPLC-MS/MS. Chem Biol Interact. 2019 Sep 1;310:108744. doi: 10.1016/j.cbi.2019.108744. Epub 2019 Jul 9.
17 Human recombinant cytochrome P450 enzymes display distinct hydrogen peroxide generating activities during substrate independent NADPH oxidase reactions. Toxicol Sci. 2014 Oct;141(2):344-52. doi: 10.1093/toxsci/kfu133. Epub 2014 Jul 24.
18 Cytochrome P450 2D6 genotype and steady state plasma levels of risperidone and 9-hydroxyrisperidone. Psychopharmacology (Berl). 1999 Dec;147(3):300-5. doi: 10.1007/s002130051171.
19 Effect of penicillin-based antibiotics, amoxicillin, ampicillin, and piperacillin, on drug-metabolizing activities of human hepatic cytochromes P450. J Toxicol Sci. 2016 Feb;41(1):143-6.
20 Cannabidiol, a major phytocannabinoid, as a potent atypical inhibitor for CYP2D6. Drug Metab Dispos. 2011 Nov;39(11):2049-56. doi: 10.1124/dmd.111.041384. Epub 2011 Aug 5.
21 Identification of human P450 isoforms involved in the metabolism of the antiallergic drug, oxatomide, and its kinetic parameters and inhibition constants. Biol Pharm Bull. 2005 Feb;28(2):328-34.
22 Pharmacokinetics of desipramine HCl when administered with cinacalcet HCl. Eur J Clin Pharmacol. 2007 Feb;63(2):159-63.
23 Effects of capsaicin and dihydrocapsaicin on human and rat liver microsomal CYP450 enzyme activities in vitro and in vivo. J Asian Nat Prod Res. 2012;14(4):382-95.
24 Inhibition of cytochrome P4502D6 activity with paroxetine normalizes the ultrarapid metabolizer phenotype as measured by nortriptyline pharmacokinetics and the debrisoquin test. Clin Pharmacol Ther. 2001 Oct;70(4):327-35.
25 Interaction of buprenorphine and its metabolite norbuprenorphine with cytochromes p450 in vitro. Drug Metab Dispos. 2003 Jun;31(6):768-72.
26 Comparative effects of thiazolidinediones on in vitro P450 enzyme induction and inhibition. Drug Metab Dispos. 2003 Apr;31(4):439-46.
27 Potential of pranlukast and zafirlukast in the inhibition of human liver cytochrome P450 enzymes. Xenobiotica. 2004 May;34(5):429-38.
28 The inhibitory effect of polyunsaturated fatty acids on human CYP enzymes. Life Sci. 2006 Nov 25;79(26):2432-40.
29 Inhibition of cytochrome P450 enzymes participating in p-nitrophenol hydroxylation by drugs known as CYP2E1 inhibitors. Chem Biol Interact. 2004 Apr 15;147(3):331-40.
30 Cytochrome P450 inhibition potential of new psychoactive substances of the tryptamine class. Toxicol Lett. 2016 Jan 22;241:82-94.
31 Stiripentol. Expert Opin Investig Drugs. 2005 Jul;14(7):905-11.
32 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
33 Cannabidiol enhances cytotoxicity of anti-cancer drugs in human head and neck squamous cell carcinoma. Sci Rep. 2020 Nov 26;10(1):20622. doi: 10.1038/s41598-020-77674-y.
34 Evidence of securin-mediated resistance to gefitinib-induced apoptosis in human cancer cells. Chem Biol Interact. 2013 Apr 25;203(2):412-22. doi: 10.1016/j.cbi.2013.03.011. Epub 2013 Mar 22.
35 Cigarette smoke and asbestos activate poly-ADP-ribose polymerase in alveolar epithelial cells. J Investig Med. 2001 Jan;49(1):68-76. doi: 10.2310/6650.2001.34092.
36 Apoptotic signaling pathways induced by nitric oxide in human lymphoblastoid cells expressing wild-type or mutant p53. Cancer Res. 2004 May 1;64(9):3022-9. doi: 10.1158/0008-5472.can-03-1880.
37 The antidepressants imipramine, clomipramine, and citalopram induce apoptosis in human acute myeloid leukemia HL-60 cells via caspase-3 activation. J Biochem Mol Toxicol. 1999;13(6):338-47. doi: 10.1002/(sici)1099-0461(1999)13:6<338::aid-jbt8>3.0.co;2-7.
38 Ciprofloxacin mediated cell growth inhibition, S/G2-M cell cycle arrest, and apoptosis in a human transitional cell carcinoma of the bladder cell line. Clin Cancer Res. 2000 Mar;6(3):891-900.
39 Investigation of molecular mechanisms underlying the antiproliferative effects of colchicine against PC3 prostate cancer cells. Toxicol In Vitro. 2021 Jun;73:105138. doi: 10.1016/j.tiv.2021.105138. Epub 2021 Mar 6.
40 Sulindac enhances adenoviral vector expressing mda-7/IL-24-mediated apoptosis in human lung cancer. Mol Cancer Ther. 2005 Feb;4(2):291-304.
41 Methotrexate induces poly(ADP-ribose) polymerase-dependent, caspase 3-independent apoptosis in subsets of proliferating CD4+ T cells. Clin Exp Immunol. 2007 May;148(2):288-95. doi: 10.1111/j.1365-2249.2007.03335.x. Epub 2007 Feb 7.
42 4.8% sevoflurane induces activation of autophagy in human neuroblastoma SH-SY5Y cells by the AMPK/mTOR signaling pathway. Neurotoxicology. 2022 May;90:256-264. doi: 10.1016/j.neuro.2022.04.008. Epub 2022 Apr 23.
43 Enhanced chemotherapeutic efficacy of docetaxel in human lung cancer cell line via GLUT1 inhibitor. J Biochem Mol Toxicol. 2023 Jun;37(6):e23348. doi: 10.1002/jbt.23348. Epub 2023 Mar 31.
44 Breast cancer cells response to the antineoplastic agents cisplatin, carboplatin, and doxorubicin at the mRNA expression levels of distinct apoptosis-related genes, including the new member, BCL2L12. Ann N Y Acad Sci. 2007 Jan;1095:35-44. doi: 10.1196/annals.1397.005.
45 Extracellular signal-regulated kinase activation and Bcl-2 downregulation mediate apoptosis after gemcitabine treatment partly via a p53-independent pathway. Eur J Pharmacol. 2004 Oct 19;502(3):169-83. doi: 10.1016/j.ejphar.2004.09.006.
46 Verapamil potentiates anti-glioblastoma efficacy of temozolomide by modulating apoptotic signaling. Toxicol In Vitro. 2018 Oct;52:306-313. doi: 10.1016/j.tiv.2018.07.001. Epub 2018 Jul 9.
47 Inhibition of caspase-dependent mitochondrial permeability transition protects airway epithelial cells against mustard-induced apoptosis. Apoptosis. 2006 Sep;11(9):1545-59. doi: 10.1007/s10495-006-8764-1.
48 Sertraline, an antidepressant, induces apoptosis in hepatic cells through the mitogen-activated protein kinase pathway. Toxicol Sci. 2014 Feb;137(2):404-15. doi: 10.1093/toxsci/kft254. Epub 2013 Nov 5.
49 -Carotene Induces Apoptosis in Human Esophageal Squamous Cell Carcinoma Cell Lines via the Cav-1/AKT/NF-B Signaling Pathway. J Biochem Mol Toxicol. 2016 Mar;30(3):148-57. doi: 10.1002/jbt.21773. Epub 2016 Jan 6.
50 Different apoptosis ratios and gene expressions in two human cell lines after sevoflurane anaesthesia. Acta Anaesthesiol Scand. 2009 Oct;53(9):1192-9. doi: 10.1111/j.1399-6576.2009.02036.x. Epub 2009 Jun 30.
51 [Mechanisms underlying the effect of arsenic trioxide on proliferation inhibition and apoptosis induction in myeloma cell line u266]. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2007 Oct;15(5):982-5.
52 Lovastatin lactone elicits human lung cancer cell apoptosis via a COX-2/PPAR-dependent pathway. Oncotarget. 2016 Mar 1;7(9):10345-62. doi: 10.18632/oncotarget.7213.
53 Induction of apoptosis by cidofovir in human papillomavirus (HPV)-positive cells. Oncol Res. 2000;12(9-10):397-408. doi: 10.3727/096504001108747855.
54 Comparison of burst of reactive oxygen species and activation of caspase-3 in apoptosis of K562 and HL-60 cells induced by docetaxel. Cancer Lett. 2004 Oct 8;214(1):103-13. doi: 10.1016/j.canlet.2004.03.047.
55 Induction of mitochondrial manganese superoxide dismutase confers resistance to apoptosis in acute myeloblastic leukaemia cells exposed to etoposide. Br J Haematol. 2000 Mar;108(3):574-81. doi: 10.1046/j.1365-2141.2000.01852.x.
56 Cisplatin-enhanced sensitivity of glioblastoma multiforme U251 cells to adenovirus-delivered TRAIL in vitro. Tumour Biol. 2010 Dec;31(6):613-22. doi: 10.1007/s13277-010-0077-x. Epub 2010 Jul 11.
57 Insulin-like growth factor I is the key growth factor in serum that protects neuroblastoma cells from hyperosmotic-induced apoptosis. J Cell Physiol. 2000 Jan;182(1):24-32. doi: 10.1002/(SICI)1097-4652(200001)182:1<24::AID-JCP3>3.0.CO;2-6.
58 mRNA expression analysis of a variety of apoptosis-related genes, including the novel gene of the BCL2-family, BCL2L12, in HL-60 leukemia cells after treatment with carboplatin and doxorubicin. Biol Chem. 2004 Nov;385(11):1099-103. doi: 10.1515/BC.2004.143.
59 Neurokinin-1 receptor (NK1R) inhibition sensitizes APL cells to anti-tumor effect of arsenic trioxide via restriction of NF-B axis: Shedding new light on resistance to Aprepitant. Int J Biochem Cell Biol. 2018 Oct;103:105-114. doi: 10.1016/j.biocel.2018.08.010. Epub 2018 Aug 23.