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

General Information of Drug (ID: DM42PFT)

Drug Name
E-3810 Drug Info
Synonyms Lucitanib; AL-3810; E-3810, EOS
Indication
Disease Entry ICD 11 Status REF
Solid tumour/cancer 2A00-2F9Z Phase 3 [1] , [2]
Cross-matching ID
PubChem CID
25031915
ChEBI ID
CHEBI:65209
CAS Number
CAS 1058137-23-7
TTD Drug ID
DM42PFT

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Patented Agent(s)
Download the Complete Related Drug List
Drug(s) Targeting Vascular endothelial growth factor receptor 3 (FLT-4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tivozanib DMUKC5L Renal cell carcinoma 2C90 Approved [4]
Sulfatinib DMPOTM4 Neuroendocrine cancer 2B72.1 Phase 3 [5]
Fruquintinib DMHOSCQ Solid tumour/cancer 2A00-2F9Z Phase 3 [6]
PI-88 DMGZPX6 Hepatocellular carcinoma 2C12.02 Phase 3 [7]
Taberminogene vadenovec DMW5PHL Vascular restinosis BE2Z Phase 3 [8]
ABT-869 DMREDYP Solid tumour/cancer 2A00-2F9Z Phase 3 [9]
MGCD516 DM752PU Solid tumour/cancer 2A00-2F9Z Phase 2/3 [10]
Famitinib DMSFWT7 Solid tumour/cancer 2A00-2F9Z Phase 2 [11]
VATALANIB DMY0UEQ Solid tumour/cancer 2A00-2F9Z Phase 2 [12]
MK-2461 DM21WBH Alzheimer disease 8A20 Phase 1/2 [13]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Fibroblast growth factor receptor 1 (FGFR1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [14]
Intedanib DMSTA36 Colorectal cancer 2B91.Z Approved [15]
Pemigatinib DM819JF Cholangiocarcinoma 2C12.10 Approved [16]
Sulfatinib DMPOTM4 Neuroendocrine cancer 2B72.1 Phase 3 [5]
Rosiglitazone + metformin DMPIDXT Diabetic complication 5A2Y Phase 3 [17]
BGJ398 DMNKBEC Cholangiocarcinoma 2C12.10 Phase 3 [18]
ARQ-087 DM02BVQ Intrahepatic cholangiocarcinoma 2C12.10 Phase 3 [19]
AZD4547 DM3827C Solid tumour/cancer 2A00-2F9Z Phase 2/3 [20]
Debio 1347 DMZW50O Solid tumour/cancer 2A00-2F9Z Phase 2 [21]
AM-001 DMGVQI8 Actinic keratosis EK90.0 Phase 2 [22]
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Drug(s) Targeting Platelet-derived growth factor receptor alpha (PDGFRA)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [23]
Ripretinib DM958QB Gastrointestinal stromal tumour 2B5B Approved [24]
Olaratumab DMNYOIX Soft tissue sarcoma 2B57 Approved [25]
Avapritinib DMK2GZX Gastrointestinal stromal tumour 2B5B Approved [26]
CP-868596 DMZIM37 Gastrointestinal cancer 2C11 Phase 3 [27]
Famitinib DMSFWT7 Solid tumour/cancer 2A00-2F9Z Phase 2 [11]
XL-820 DMMHX9K Solid tumour/cancer 2A00-2F9Z Phase 2 [28]
MP470 DMELUAK Solid tumour/cancer 2A00-2F9Z Phase 2 [29]
MEDI-575 DMI9WVM Glioblastoma multiforme 2A00.0 Phase 2 [30]
Pyridine derivative 18 DMBZMYT N. A. N. A. Patented [31]
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Drug(s) Targeting Fibroblast growth factor receptor 2 (FGFR2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Pemigatinib DM819JF Cholangiocarcinoma 2C12.10 Approved [16]
Interferon Alfa-2a, Recombinant DMUTZ8S Chronic HCV-1 infection 1E51.1 Approved [32]
Palifermin DM9JOYP Oral mucositis DA01.11 Approved [33]
Trafermin DMLKI2B Periodontitis DA0C Phase 3 [34]
Debio 1347 DMZW50O Solid tumour/cancer 2A00-2F9Z Phase 2 [21]
LY2874455 DMZ0DMY Solid tumour/cancer 2A00-2F9Z Phase 2 [35]
MK-2461 DM21WBH Alzheimer disease 8A20 Phase 1/2 [13]
AEE-788 DMEOS5K Solid tumour/cancer 2A00-2F9Z Phase 1/2 [17]
BAY1179470 DM7L91K Solid tumour/cancer 2A00-2F9Z Phase 1 [36]
Alofanib DMIEKTF Gastric adenocarcinoma 2B72 Phase 1 [37]
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Drug(s) Targeting Platelet-derived growth factor receptor beta (PDGFRB)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sorafenib DMS8IFC Hepatocellular carcinoma 2C12.02 Approved [38]
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [23]
Becaplermin DM1R5X4 Diabetic complication 5A2Y Approved [39]
Famitinib DMSFWT7 Solid tumour/cancer 2A00-2F9Z Phase 2 [11]
XL-820 DMMHX9K Solid tumour/cancer 2A00-2F9Z Phase 2 [28]
MK-2461 DM21WBH Alzheimer disease 8A20 Phase 1/2 [13]
SNN-0031 DM2X3BR Brain injury NA07.Z Phase 1/2 [40]
TAK-593 DMNFZOT Solid tumour/cancer 2A00-2F9Z Phase 1 [41]
Pyridine derivative 18 DMBZMYT N. A. N. A. Patented [31]
PMID25656651-Compound-21a DMCKAON N. A. N. A. Patented [42]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Vascular endothelial growth factor receptor 1 (FLT-1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tivozanib DMUKC5L Renal cell carcinoma 2C90 Approved [4]
Sulfatinib DMPOTM4 Neuroendocrine cancer 2B72.1 Phase 3 [5]
Fruquintinib DMHOSCQ Solid tumour/cancer 2A00-2F9Z Phase 3 [6]
Famitinib DMSFWT7 Solid tumour/cancer 2A00-2F9Z Phase 2 [11]
X-82 DMW1NKO Age-related macular degeneration 9B75.0 Phase 2 [43]
OCV-101 DMT9QI2 Pancreatic cancer 2C10 Phase 2 [44]
LY3012212 DMRVEHY Arteriosclerosis BD40 Phase 2 [45]
OTSGC-A24 DMN0ZQ5 Colorectal cancer 2B91.Z Phase 1/2 [46]
CEP-11981 DMYDTJ6 Solid tumour/cancer 2A00-2F9Z Phase 1 [47]
EW-A-401 DM3VC6T Peripheral vascular disease BD4Z Phase 1 [48]
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Drug(s) Targeting Vascular endothelial growth factor receptor 2 (KDR)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sorafenib DMS8IFC Hepatocellular carcinoma 2C12.02 Approved [38]
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [14]
Regorafenib DMHSY1I Metastatic colorectal cancer 2B91 Approved [49]
Sunitinib DMCBJSR Gastrointestinal cancer 2C11 Approved [50]
Axitinib DMGVH6N Renal cell carcinoma 2C90 Approved [51]
Vandetanib DMRICNP Solid tumour/cancer 2A00-2F9Z Approved [17]
Pazopanib HCl DM6U9CQ Renal cell carcinoma 2C90 Approved [52]
Cabozantinib DMIYDT4 Thyroid cancer 2D10 Approved [53]
Tivozanib DMUKC5L Renal cell carcinoma 2C90 Approved [4]
Lenvatinib DMB1IU4 Thyroid cancer 2D10 Approved [54]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Fibroblast growth factor receptor 3 (FGFR3)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Pemigatinib DM819JF Cholangiocarcinoma 2C12.10 Approved [16]
Trapidil DMY67U8 Acute coronary syndrome BA41 Phase 4 [55]
TKI258 DMYLT67 Renal cell carcinoma 2C90 Phase 3 [17]
BMS-582664 DMDAN8H Hepatocellular carcinoma 2C12.02 Phase 3 [17]
Debio 1347 DMZW50O Solid tumour/cancer 2A00-2F9Z Phase 2 [21]
B-701 DMOMDA4 Bladder cancer 2C94 Phase 2 [56]
Recifercept DML8N3Y Achondroplasia LD24.00 Phase 2 [57]
MK-2461 DM21WBH Alzheimer disease 8A20 Phase 1/2 [13]
AEE-788 DMEOS5K Solid tumour/cancer 2A00-2F9Z Phase 1/2 [17]
Anti-FGFR3 DM6QENU Multiple myeloma 2A83 Phase 1 [58]
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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
Fibroblast growth factor receptor 1 (FGFR1) TTRLW2X FGFR1_HUMAN Inhibitor [3]
Fibroblast growth factor receptor 2 (FGFR2) TTGJVQM FGFR2_HUMAN Inhibitor [3]
Fibroblast growth factor receptor 3 (FGFR3) TTST7KB FGFR3_HUMAN Inhibitor [3]
Platelet-derived growth factor receptor alpha (PDGFRA) TT8FYO9 PGFRA_HUMAN Inhibitor [3]
Platelet-derived growth factor receptor beta (PDGFRB) TTI7421 PGFRB_HUMAN Inhibitor [3]
Vascular endothelial growth factor receptor 1 (FLT-1) TT2Q6G1 VGFR1_HUMAN Inhibitor [3]
Vascular endothelial growth factor receptor 2 (KDR) TTUTJGQ VGFR2_HUMAN Inhibitor [3]
Vascular endothelial growth factor receptor 3 (FLT-4) TTDCBX5 VGFR3_HUMAN Inhibitor [3]

References

1 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: 7649).
2 ClinicalTrials.gov (NCT02135107) A Double-blind Comparative Study of the Efficacy and Safety of E3810 10mg Once and Twice Daily in Maintenance Therapy for PPI Resistant Gastroesophageal Reflux Disease Patients. U.S. National Institutes of Health.
3 E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011 Feb 15;71(4):1396-405.
4 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services
5 Clinical pipeline report, company report or official report of Hutchison Medi Pharma.
6 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.
7 Company report (Medigen)
8 Advances in kinase targeting: current clinical use and clinical trials. Trends Pharmacol Sci. 2014 Nov;35(11):604-20.
9 Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor. Mol Cancer Ther. 2006 Apr;5(4):995-1006.
10 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: 1814).
11 Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
12 Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors. J Med Chem. 2005 Mar 10;48(5):1610-9.
13 MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
14 Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
15 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
16 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
17 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.
18 Pharmacological inhibition of fibroblast growth factor (FGF) receptor signaling ameliorates FGF23-mediated hypophosphatemic rickets. J Bone Miner Res. 2013 Apr;28(4):899-911.
19 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: 1808).
20 AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family. Cancer Res. 2012 Apr 15;72(8):2045-56.
21 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
22 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029917)
23 Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel... J Med Chem. 2003 Mar 27;46(7):1116-9.
24 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
25 A phase I study of olaratumab, an anti-platelet-derived growth factor receptor alpha (PDGFRalpha) monoclonal antibody, in patients with advanced solid tumors. Cancer Chemother Pharmacol. 2014 Mar;73(3):595-604.
26 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
27 The FLT3 and PDGFR inhibitor crenolanib is a substrate of the multidrug resistance protein ABCB1 but does not inhibit transport function at pharmacologically relevant concentrations.Invest New Drugs.2015 Apr;33(2):300-9.
28 National Cancer Institute Drug Dictionary (drug id 452042).
29 Phase 1B study of amuvatinib in combination with five standard cancer therapies in adults with advanced solid tumors. Cancer Chemother Pharmacol. 2014 Jul;74(1):195-204.
30 Clinical pipeline report, company report or official report of MedImmune (2011).
31 RET kinase inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jan;27(1):91-99.
32 DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue):D901-6.
33 Keratinocyte growth factor. Expert Opin Biol Ther. 2009 Jun;9(6):779-87.
34 Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24.
35 Company report (Eli Lilly) (drug: LY2874455)
36 National Cancer Institute Drug Dictionary (drug id 751593).
37 Corrigendum to 'Targeting FGFR2 with alofanib (RPT835) shows potent activity in tumour models' [Eur J Cancer 61 (2016) 20-28]. Eur J Cancer. 2017 Jan;70:156.
38 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.
39 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
40 Company report (Neuronova)
41 Biochemical characterization of TAK-593, a novel VEGFR/PDGFR inhibitor with a two-step slow binding mechanism. Biochemistry. 2011 Feb 8;50(5):738-51.
42 Bcr-Abl tyrosine kinase inhibitors: a patent review.Expert Opin Ther Pat. 2015 Apr;25(4):397-412.
43 National Cancer Institute Drug Dictionary (drug id 695817).
44 Phase I trial of OTS11101, an anti-angiogenic vaccine targeting vascular endothelial growth factor receptor 1 in solid tumor.Cancer Sci.2013 Jan;104(1):98-104.
45 Icrucumab, a fully human monoclonal antibody against the vascular endothelial growth factor receptor-1, in the treatment of patients with advanced solid malignancies: a Phase 1 study. Invest New Drugs. 2014 Apr;32(2):303-11.
46 J Clin Oncol 33, 2015 (suppl 3; abstr 65).
47 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: 8189).
48 DOI: http://dx.doi.org/10.1016/j.tips.2014.09.007
49 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
50 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
51 Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
52 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
53 Clinical pipeline report, company report or official report of Exelixis (2011).
54 Emerging drugs for ovarian cancer. Expert Opin Emerg Drugs. 2008 Sep;13(3):523-36.
55 Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
56 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
57 In vitro and in vivo characterization of Recifercept, a soluble fibroblast growth factor receptor 3, as treatment for achondroplasia. PLoS One. 2020 Dec 28;15(12):e0244368.
58 Clinical pipeline report, company report or official report of Genentech (2011).