General Information of Drug (ID: DMHJTR2)

Drug Name
XL880 Drug Info
Synonyms GSK 089; GSK 1363089; GSK1363089; XL 880; GSK1363089, GSK089, foretinib, EXEL-2880, XL880; 88Z; MET inhibitors
Indication
Disease Entry ICD 11 Status REF
Breast cancer 2C60-2C65 Phase 2 [1]
Gastric adenocarcinoma 2B72 Phase 2 [2]
Renal cell carcinoma 2C90 Phase 2 [2]
Squamous head and neck cell carcinom 2D60.0 Phase 2 [2]
Solid tumour/cancer 2A00-2F9Z Phase 1 [2]
Therapeutic Class
Anticancer Agents
Cross-matching ID
PubChem CID
42642645
ChEBI ID
CHEBI:91418
CAS Number
CAS 849217-64-7
TTD Drug ID
DMHJTR2

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug(s) Targeting Proto-oncogene c-Met (MET)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Crizotinib DM4F29C Non-small-cell lung cancer 2C25.Y Approved [6]
Cabozantinib DMIYDT4 Medullary thyroid gland carcinoma Approved [7]
Amivantamab DMZ7AMY Non-small-cell lung cancer 2C25 Approved [8]
Capmatinib DMYCXKL Non-small-cell lung cancer 2C25.Y Approved [9]
Tepotinib DMUQ0E8 Non-small-cell lung cancer 2C25 Approved [10]
RG3638 DMTQJE0 Gastric adenocarcinoma 2B72 Phase 3 [11]
Savolitinib DMALFKX Renal cell carcinoma 2C90 Phase 3 [12]
Beperminogene perplasmid DM6RWBN Critical limb ischemia BD4Y Phase 3 [13]
Tivantinib DMNVP8Q Hepatocellular carcinoma 2C12.02 Phase 3 [14]
MGCD516 DM752PU Solid tumour/cancer 2A00-2F9Z Phase 2/3 [11]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [15]
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [16]
Regorafenib DMHSY1I Gastrointestinal stromal tumour 2B5B Approved [6]
Sunitinib DMCBJSR Acute undifferentiated leukemia Approved [17]
Axitinib DMGVH6N Renal cell carcinoma 2C90 Approved [18]
Vandetanib DMRICNP Solid tumour/cancer 2A00-2F9Z Approved [19]
Pazopanib HCl DM6U9CQ Renal cell carcinoma 2C90 Approved [20]
Fruquintinib DMHOSCQ Colorectal cancer 2B91.Z Approved [21]
Cabozantinib DMIYDT4 Medullary thyroid gland carcinoma Approved [7]
Tivozanib DMUKC5L Renal cell carcinoma 2C90 Approved [22]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cabozantinib DMIYDT4 Medullary thyroid gland carcinoma Approved [23]
Crizotinib DM4F29C Non-small-cell lung cancer 2C25.Y Approved [24]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [25]
Lumiracoxib DM1S4AG Chronic renal failure GB61.Z Approved [25]
Clavulanate DM2FGRT Bacteremia 1A73 Approved [25]
Methotrexate DM2TEOL Anterior urethra cancer Approved [26]
Quercetin DM3NC4M Obesity 5B81 Approved [27]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [25]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [28]
Methylprednisolone DM4BDON Acute adrenal insufficiency Approved [26]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Bosutinib DMTI8YE Blast phase chronic myelogenous leukemia, BCR-ABL1 positive Approved [29]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [30]
Methotrexate DM2TEOL Anterior urethra cancer Approved [31]
Quercetin DM3NC4M Obesity 5B81 Approved [32]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [33]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [34]
Plicamycin DM7C8YV Hypercalcaemia 5B91.0 Approved [35]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [36]
Sevoflurane DMC9O43 Anaesthesia 9A78.6 Approved [36]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [37]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Selenium DM25CGV N. A. N. A. Approved [38]
Dactinomycin DM2YGNW Adult kidney Wilms tumor Approved [39]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [40]
Quercetin DM3NC4M Obesity 5B81 Approved [27]
Cyclophosphamide DM4O2Z7 Advanced cancer 2A00-2F9Z Approved [39]
Plicamycin DM7C8YV Hypercalcaemia 5B91.0 Approved [41]
Leflunomide DMR8ONJ Arthritis FA20 Approved [42]
Clodronate DM9Y6X7 Hypercalcaemia 5B91.0 Approved [43]
Cidofovir DMA13GD Cytomegalovirus infection 1D82 Approved [43]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [43]
⏷ 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
Proto-oncogene c-Met (MET) TTNDSF4 MET_HUMAN Modulator [3]
Vascular endothelial growth factor receptor 2 (KDR) TTUTJGQ VGFR2_HUMAN Modulator [3]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Hepatocyte growth factor receptor (MET) OT7K55MU MET_HUMAN Post-Translational Modifications [4]
Proto-oncogene tyrosine-protein kinase Src (SRC) OTETYX40 SRC_HUMAN Post-Translational Modifications [4]
Tyrosine-protein kinase receptor UFO (AXL) OTKA2SUX UFO_HUMAN Gene/Protein Processing [5]

References

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3 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
4 LRIG1 modulates cancer cell sensitivity to Smac mimetics by regulating TNF expression and receptor tyrosine kinase signaling. Cancer Res. 2012 Mar 1;72(5):1229-38. doi: 10.1158/0008-5472.CAN-11-2428. Epub 2012 Jan 12.
5 Activation of the AXL kinase causes resistance to EGFR-targeted therapy in lung cancer. Nat Genet. 2012 Jul 1;44(8):852-60. doi: 10.1038/ng.2330.
6 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
7 Clinical pipeline report, company report or official report of Exelixis (2011).
8 Antitumor Activity of Amivantamab (JNJ-61186372), an EGFR-MET Bispecific Antibody, in Diverse Models of EGFR Exon 20 Insertion-Driven NSCLC. Cancer Discov. 2020 Aug;10(8):1194-1209.
9 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
10 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2021
11 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1815).
12 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
13 Beperminogene perplasmid for the treatment of critical limb ischemia. Expert Rev Cardiovasc Ther. 2014 Oct;12(10):1145-56.
14 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7948).
15 Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling.Mol Cancer Ther.2008 Oct;7(10):3129-40.
16 Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
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19 A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
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21 Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy. Cancer Biol Ther. 2014;15(12):1635-45.
22 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services
23 ROS-dependent DNA damage contributes to crizotinib-induced hepatotoxicity via the apoptotic pathway. Toxicol Appl Pharmacol. 2019 Nov 15;383:114768. doi: 10.1016/j.taap.2019.114768. Epub 2019 Oct 19.
24 Antitumor action of the MET tyrosine kinase inhibitor crizotinib (PF-02341066) in gastric cancer positive for MET amplification. Mol Cancer Ther. 2012 Jul;11(7):1557-64. doi: 10.1158/1535-7163.MCT-11-0934. Epub 2012 Jun 22.
25 An in vitro coculture system of human peripheral blood mononuclear cells with hepatocellular carcinoma-derived cells for predicting drug-induced liver injury. Arch Toxicol. 2021 Jan;95(1):149-168. doi: 10.1007/s00204-020-02882-4. Epub 2020 Aug 20.
26 Antirheumatic drug response signatures in human chondrocytes: potential molecular targets to stimulate cartilage regeneration. Arthritis Res Ther. 2009;11(1):R15.
27 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.
28 All-trans retinoic acid inhibits the cell proliferation but enhances the cell invasion through up-regulation of c-met in pancreatic cancer cells. Cancer Lett. 2005 Jun 28;224(2):303-10. doi: 10.1016/j.canlet.2004.10.016. Epub 2004 Dec 8.
29 SKI-606 decreases growth and motility of colorectal cancer cells by preventing pp60(c-Src)-dependent tyrosine phosphorylation of beta-catenin and its nuclear signaling. Cancer Res. 2006 Feb 15;66(4):2279-86. doi: 10.1158/0008-5472.CAN-05-2057.
30 Selective activation of Src family kinases and JNK by low levels of chromium(VI). Toxicol Appl Pharmacol. 2003 Aug 1;190(3):214-23. doi: 10.1016/s0041-008x(03)00188-1.
31 The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
32 Quercetin exerts anti-melanoma activities and inhibits STAT3 signaling. Biochem Pharmacol. 2014 Feb 1;87(3):424-34. doi: 10.1016/j.bcp.2013.11.008. Epub 2013 Nov 23.
33 Essential role of cell cycle regulatory genes p21 and p27 expression in inhibition of breast cancer cells by arsenic trioxide. Med Oncol. 2011 Dec;28(4):1225-54.
34 Dehydroepiandrosterone Activation of G-protein-coupled Estrogen Receptor Rapidly Stimulates MicroRNA-21 Transcription in Human Hepatocellular Carcinoma Cells. J Biol Chem. 2015 Jun 19;290(25):15799-15811. doi: 10.1074/jbc.M115.641167. Epub 2015 May 11.
35 Mithramycin inhibits human epithelial carcinoma cell proliferation and migration involving downregulation of Eps8 expression. Chem Biol Interact. 2010 Jan 5;183(1):181-6. doi: 10.1016/j.cbi.2009.09.018.
36 The differential cancer growth associated with anaesthetics in a cancer xenograft model of mice: mechanisms and implications of postoperative cancer recurrence. Cell Biol Toxicol. 2023 Aug;39(4):1561-1575. doi: 10.1007/s10565-022-09747-9. Epub 2022 Aug 12.
37 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.
38 Selenium and vitamin E: cell type- and intervention-specific tissue effects in prostate cancer. J Natl Cancer Inst. 2009 Mar 4;101(5):306-20.
39 Genomic profiling uncovers a molecular pattern for toxicological characterization of mutagens and promutagens in vitro. Toxicol Sci. 2011 Jul;122(1):185-97.
40 Simvastatin inactivates beta1-integrin and extracellular signal-related kinase signaling and inhibits cell proliferation in head and neck squamous cell carcinoma cells. Cancer Sci. 2007 Jun;98(6):890-9.
41 The human receptor tyrosine kinase Axl gene--promoter characterization and regulation of constitutive expression by Sp1, Sp3 and CpG methylation. Biosci Rep. 2008 Jun;28(3):161-76. doi: 10.1042/BSR20080046.
42 Endoplasmic reticulum stress and MAPK signaling pathway activation underlie leflunomide-induced toxicity in HepG2 Cells. Toxicology. 2017 Dec 1;392:11-21.
43 Transcriptomics hit the target: monitoring of ligand-activated and stress response pathways for chemical testing. Toxicol In Vitro. 2015 Dec 25;30(1 Pt A):7-18.