General Information of Drug (ID: DMOKUA5)

Drug Name
XR-5000 Drug Info
Synonyms DACA; SN-22995
Indication
Disease Entry ICD 11 Status REF
Colorectal cancer 2B91.Z Phase 2 [1]
Cross-matching ID
PubChem CID
107805
TTD Drug ID
DMOKUA5

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug(s) Targeting DNA topoisomerase I (TOP1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Irinotecan DMP6SC2 Adenocarcinoma 2D40 Approved [4]
Topotecan DMP6G8T Central nervous system neoplasm Approved [4]
B-Lactams DMR8YD6 Bacterial infection 1A00-1C4Z Approved [5]
Belotecan hydrocholoride DM3SRJZ Small-cell lung cancer 2C25.Y Approved [6]
Topetecan DMAE6LK Small-cell lung cancer 2C25.Y Approved [7]
Karenitecin DMCRGY4 Lung cancer 2C25.0 Phase 3 [8]
Camptothecin DM6CHNJ Solid tumour/cancer 2A00-2F9Z Phase 3 [9]
Exatecan DMCA7FN Solid tumour/cancer 2A00-2F9Z Phase 3 [10]
Edotecarin DM3ZL7D Gastric adenocarcinoma 2B72 Phase 3 [11]
Rubitecan DMDWU1S Human immunodeficiency virus infection 1C62 Phase 3 [12]
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Drug(s) Targeting DNA topoisomerase II (TOP2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [4]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [13]
Teniposide DMLW57T Acute lymphoblastic leukaemia 2A85 Approved [4]
Mitoxantrone DMM39BF Acute myelogenous leukaemia 2A41 Approved [14]
Idarubicin DMM0XGL Acute myelogenous leukaemia 2A41 Approved [4]
Epirubicin DMPDW6T Solid tumour/cancer 2A00-2F9Z Approved [4]
Lomefloxacin DMVRH9C Bacterial infection 1A00-1C4Z Approved [15]
Dexrazoxane DMD7X1O Breast cancer 2C60-2C65 Approved [4]
Podofilox DMT2EJP Condyloma 1A95 Approved [16]
Enoxacin DMYTE6L Acute gonococcal cervicitis Approved [17]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Albumin (ALB)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [18]
Sulfamethoxazole DMB08GE Acute otitis media AB00 Approved [19]
Tolbutamide DM02AWV Advanced cancer 2A00-2F9Z Approved [20]
Diazepam DM08E9O Alcohol withdrawal Approved [21]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [22]
Methimazole DM25FL8 Hyperthyroidism 5A02 Approved [23]
Imipramine DM2NUH3 Depression 6A70-6A7Z Approved [24]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [25]
Methotrexate DM2TEOL Anterior urethra cancer Approved [26]
Quercetin DM3NC4M Obesity 5B81 Approved [27]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Aldehyde oxidase (AOX1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL Anterior urethra cancer Approved [28]
Quercetin DM3NC4M Obesity 5B81 Approved [29]
Rofecoxib DM3P5DA Osteoarthritis FA00-FA05 Approved [30]
Methylprednisolone DM4BDON Acute adrenal insufficiency Approved [31]
Nefazodone DM4ZS8M Major depressive disorder 6A70.3 Approved [32]
Panobinostat DM58WKG Chronic graft versus host disease Approved [33]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [34]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [35]
Dasatinib DMJV2EK Blast phase chronic myelogenous leukemia, BCR-ABL1 positive Approved [36]
Temozolomide DMKECZD Adenocarcinoma 2D40 Approved [37]
⏷ 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
DNA topoisomerase I (TOP1) TTGTQHC TOP1_HUMAN Modulator [1]
DNA topoisomerase II (TOP2) TT0IHXV TOP2A_HUMAN; TOP2B_HUMAN Modulator [1]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Albumin (ALB) OTVMM513 ALBU_HUMAN Protein Interaction/Cellular Processes [2]
Aldehyde oxidase (AOX1) OT2FZP6H AOXA_HUMAN Regulation of Drug Effects [3]

References

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2 Effects of protein binding on the in vitro activity of antitumour acridine derivatives and related anticancer drugs. Cancer Chemother Pharmacol. 2000;45(5):417-22. doi: 10.1007/s002800051011.
3 In vitro-in vivo correlation for intrinsic clearance for drugs metabolized by human aldehyde oxidase. Drug Metab Dispos. 2010 Aug;38(8):1322-7. doi: 10.1124/dmd.110.033555. Epub 2010 May 5.
4 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
5 Luteolin, an emerging anti-cancer flavonoid, poisons eukaryotic DNA topoisomerase I. Biochem J. 2002 Sep 1;366(Pt 2):653-61.
6 Impact of natural products on developing new anti-cancer agents. Chem Rev. 2009 Jul;109(7):3012-43.
7 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
8 Characterization of protein kinase chk1 essential for the cell cycle checkpoint after exposure of human head and neck carcinoma A253 cells to a novel topoisomerase I inhibitor BNP1350. Mol Pharmacol.2000 Mar;57(3):453-9.
9 Topoisomerase I inhibitors: camptothecins and beyond. Nat Rev Cancer. 2006 Oct;6(10):789-802.
10 Phase I study of topoisomerase I inhibitor exatecan mesylate (DX-8951f) given as weekly 24-hour infusions three of every four weeks. Clin Cancer Res. 2001 Dec;7(12):3963-70.
11 Edotecarin: a novel topoisomerase I inhibitor. Clin Colorectal Cancer. 2005 May;5(1):27-36.
12 Rubitecan. Expert Opin Investig Drugs. 2006 Jan;15(1):71-9.
13 Etoposide, topoisomerase II and cancer.Curr Med Chem Anticancer Agents.2005 Jul;5(4):363-72.
14 Mitoxantrone, a topoisomerase II inhibitor, induces apoptosis of B-chronic lymphocytic leukaemia cells. Br J Haematol. 1998 Jan;100(1):142-6.
15 Inhibition of human topoisomerase IIalpha by fluoroquinolones and ultraviolet A irradiation. Toxicol Sci. 2002 Sep;69(1):16-22.
16 Antitumor properties of podophyllotoxin and related compounds. Curr Pharm Des. 2000 Dec;6(18):1811-39.
17 Clinical pharmacokinetics of the newer antibacterial 4-quinolones. Clin Pharmacokinet. 1988 Feb;14(2):96-121.
18 Gene expression analysis of precision-cut human liver slices indicates stable expression of ADME-Tox related genes. Toxicol Appl Pharmacol. 2011 May 15;253(1):57-69.
19 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.
20 A protein-coated magnetic beads as a tool for the rapid drug-protein binding study. J Pharm Biomed Anal. 2010 Jul 8;52(3):420-4. doi: 10.1016/j.jpba.2009.06.023. Epub 2009 Jun 18.
21 The three recombinant domains of human serum albumin. Structural characterization and ligand binding properties. J Biol Chem. 1999 Oct 8;274(41):29303-10. doi: 10.1074/jbc.274.41.29303.
22 Exploring binding properties of sertraline with human serum albumin: Combination of spectroscopic and molecular modeling studies. Chem Biol Interact. 2015 Dec 5;242:235-46. doi: 10.1016/j.cbi.2015.10.006. Epub 2015 Oct 22.
23 Low-expressional IGF1 mediated methimazole-induced liver developmental toxicity in fetal mice. Toxicology. 2018 Sep 1;408:70-79. doi: 10.1016/j.tox.2018.07.004. Epub 2018 Jul 7.
24 Use of peak decay analysis and affinity microcolumns containing silica monoliths for rapid determination of drug-protein dissociation rates. J Chromatogr A. 2011 Apr 15;1218(15):2072-8. doi: 10.1016/j.chroma.2010.09.070. Epub 2010 Oct 16.
25 [Colchicine in chronic liver disease of alcoholic etiology. Double-blind, randomized study of its effects on blood levels of plasma proteins and clinical course in patients]. Rev Assoc Med Bras (1992). 1995 May-Jun;41(3):207-12.
26 Editor's Highlight: Modeling Compound-Induced Fibrogenesis In Vitro Using Three-Dimensional Bioprinted Human Liver Tissues. Toxicol Sci. 2016 Dec;154(2):354-367. doi: 10.1093/toxsci/kfw169. Epub 2016 Sep 7.
27 Covalent binding of the flavonoid quercetin to human serum albumin. J Agric Food Chem. 2005 May 18;53(10):4194-7. doi: 10.1021/jf050061m.
28 Global molecular effects of tocilizumab therapy in rheumatoid arthritis synovium. Arthritis Rheumatol. 2014 Jan;66(1):15-23.
29 Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
30 Rofecoxib modulates multiple gene expression pathways in a clinical model of acute inflammatory pain. Pain. 2007 Mar;128(1-2):136-47.
31 Antirheumatic drug response signatures in human chondrocytes: potential molecular targets to stimulate cartilage regeneration. Arthritis Res Ther. 2009;11(1):R15.
32 Robustness testing and optimization of an adverse outcome pathway on cholestatic liver injury. Arch Toxicol. 2020 Apr;94(4):1151-1172. doi: 10.1007/s00204-020-02691-9. Epub 2020 Mar 10.
33 A transcriptome-based classifier to identify developmental toxicants by stem cell testing: design, validation and optimization for histone deacetylase inhibitors. Arch Toxicol. 2015 Sep;89(9):1599-618.
34 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
35 Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.
36 Dasatinib reverses cancer-associated fibroblasts (CAFs) from primary lung carcinomas to a phenotype comparable to that of normal fibroblasts. Mol Cancer. 2010 Jun 27;9:168.
37 Temozolomide induces activation of Wnt/-catenin signaling in glioma cells via PI3K/Akt pathway: implications in glioma therapy. Cell Biol Toxicol. 2020 Jun;36(3):273-278. doi: 10.1007/s10565-019-09502-7. Epub 2019 Nov 22.