| Drug General Information |
| Drug ID |
D02WVT
|
| Former ID |
DIB012358
|
| Drug Name |
E-3810
|
| Synonyms |
Lucitanib; AL-3810; E-3810, EOS
|
| Drug Type |
Small molecular drug
|
| Indication |
Solid tumours [ICD9: 140-199, 210-229; ICD10:C00-D48]
|
Phase 3 |
[1],
[2]
|
|---|
| Company |
Clovis oncology
|
| Structure |
|
Download
2D MOL
3D MOL
|
| Formula |
C26H25N3O4
|
| InChI |
InChI=1S/C26H25N3O4/c1-28-25(30)19-5-3-4-16-12-17(6-7-18(16)19)33-22-8-11-29-21-14-24(23(31-2)13-20(21)22)32-15-26(27)9-10-26/h3-8,11-14H,9-10,15,27H2,1-2H3,(H,28,30)
|
| InChIKey |
CUDVHEFYRIWYQD-UHFFFAOYSA-N
|
| PubChem Compound ID |
|
| PubChem Substance ID |
56382652, 57542537, 141782498, 144115928, 152258702, 160645076, 160647536, 162108730, 163348563, 164045850, 172918938, 185990479, 198970413, 223365984, 223389506, 223471435, 225137076, 226712306, 242566533, 247047042, 248791928, 249818644, 252214555, 252478507
|
| Drug Resistance Mutation (DRM) |
| DRM |
DRM Info
|
| Target and Pathway |
| Target(s) |
Basic fibroblast growth factor receptor 1 |
Target Info |
Inhibitor |
[3]
|
|---|
| Fibroblast growth factor receptor 2 |
Target Info |
Inhibitor |
[3]
|
| Vascular endothelial growth factor receptor 2 |
Target Info |
Inhibitor |
[3]
|
| Alpha platelet-derived growth factor receptor |
Target Info |
Inhibitor |
[3]
|
| FGF-3 receptor |
Target Info |
Inhibitor |
[3]
|
| Vascular endothelial growth factor receptor 3 |
Target Info |
Inhibitor |
[3]
|
| Beta platelet-derived growth factor receptor |
Target Info |
Inhibitor |
[3]
|
| Vascular endothelial growth factor receptor 1 |
Target Info |
Inhibitor |
[3]
|
|
KEGG Pathway
|
MAPK signaling pathway
|
|
Ras signaling pathway
|
|
Rap1 signaling pathway
|
|
PI3K-Akt signaling pathway
|
|
Adherens junction
|
|
Signaling pathways regulating pluripotency of stem cells
|
|
Regulation of actin cytoskeleton
|
|
Pathways in cancer
|
|
Proteoglycans in cancer
|
|
Prostate cancer
|
|
Melanoma
|
|
Central carbon metabolism in cancerhsa04010:MAPK signaling pathway
|
|
Endocytosis
|
|
Central carbon metabolism in cancerhsa04014:Ras signaling pathway
|
|
Cytokine-cytokine receptor interaction
|
|
VEGF signaling pathway
|
|
Focal adhesion
|
|
Proteoglycans in cancerhsa04010:MAPK signaling pathway
|
|
Calcium signaling pathway
|
|
Gap junction
|
|
HTLV-I infection
|
|
MicroRNAs in cancer
|
|
Glioma
|
|
Central carbon metabolism in cancer
|
|
Choline metabolism in cancerhsa04010:MAPK signaling pathway
|
|
Bladder cancer
|
|
Focal adhesionhsa04010:MAPK signaling pathway
|
|
Choline metabolism in cancerhsa04014:Ras signaling pathway
|
|
HIF-1 signaling pathway
|
|
Transcriptional misregulation in cancer
|
|
Rheumatoid arthritis
|
|
NetPath Pathway
|
TCR Signaling PathwayNetPath_13:IL1 Signaling PathwayNetPath_14:IL2 Signaling PathwayNetPath_7:TGF_beta_Receptor Signaling PathwayNetPath_9:TNFalpha Signaling Pathway
|
|
PANTHER Pathway
|
Angiogenesis
|
|
FGF signaling pathwayP00021:FGF signaling pathwayP00005:Angiogenesis
|
|
VEGF signaling pathwayP00005:Angiogenesis
|
|
PDGF signaling pathwayP00021:FGF signaling pathwayP00005:Angiogenesis
|
|
PDGF signaling pathway
|
|
Pathway Interaction Database
|
Glypican 1 network
|
|
Syndecan-4-mediated signaling events
|
|
N-cadherin signaling events
|
|
FGF signaling pathwayfgf_pathway:FGF signaling pathwayhif2pathway:HIF-2-alpha transcription factor network
|
|
Beta3 integrin cell surface interactions
|
|
Signaling events mediated by TCPTP
|
|
SHP2 signaling
|
|
S1P1 pathway
|
|
VEGF and VEGFR signaling network
|
|
Integrins in angiogenesis
|
|
Signaling events mediated by VEGFR1 and VEGFR2
|
|
Notch-mediated HES/HEY networkatf2_pathway:ATF-2 transcription factor network
|
|
PDGFR-alpha signaling pathway
|
|
PDGF receptor signaling networkvegf_vegfr_pathway:VEGF and VEGFR signaling network
|
|
VEGFR3 signaling in lymphatic endotheliumptp1bpathway:Signaling events mediated by PTP1B
|
|
S1P3 pathway
|
|
Nectin adhesion pathway
|
|
Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling
|
|
PDGFR-beta signaling pathway
|
|
Validated targets of C-MYC transcriptional repression
|
|
PDGF receptor signaling networkglypican_1pathway:Glypican 1 network
|
|
HIF-2-alpha transcription factor network
|
|
VEGFR1 specific signals
|
|
Reactome
|
Activated point mutants of FGFR2R-HSA-194306:Neurophilin interactions with VEGF and VEGFR
|
|
VEGF binds to VEGFR leading to receptor dimerization
|
|
Integrin cell surface interactions
|
|
EPHA-mediated growth cone collapse
|
|
VEGFA-VEGFR2 Pathway
|
|
VEGFR2 mediated cell proliferationR-HSA-1257604:PIP3 activates AKT signaling
|
|
Constitutive Signaling by Aberrant PI3K in Cancer
|
|
RAF/MAP kinase cascadeR-HSA-2033514:FGFR3 mutant receptor activationR-HSA-195399:VEGF binds to VEGFR leading to receptor dimerizationR-HSA-1257604:PIP3 activates AKT signaling
|
|
RAF/MAP kinase cascadeR-HSA-194306:Neurophilin interactions with VEGF and VEGFR
|
|
WikiPathways
|
Regulation of Actin Cytoskeleton
|
|
Endochondral Ossification
|
|
MAPK Signaling Pathway
|
|
Mesodermal Commitment Pathway
|
|
Hair Follicle Development: Induction (Part 1 of 3)
|
|
Integrated Pancreatic Cancer Pathway
|
|
Signaling Pathways in Glioblastoma
|
|
Neural Crest Differentiation
|
|
Signaling by FGFRWP51:Regulation of Actin Cytoskeleton
|
|
Ectoderm Differentiation
|
|
Hair Follicle Development: Organogenesis (Part 2 of 3)
|
|
Cardiac Hypertrophic Response
|
|
Signaling by FGFR
|
|
MicroRNAs in cardiomyocyte hypertrophy
|
|
AngiogenesisWP306:Focal Adhesion
|
|
Nifedipine Activity
|
|
Cardiac Progenitor Differentiation
|
|
Signaling by VEGF
|
|
AngiogenesisWP51:Regulation of Actin Cytoskeleton
|
|
Osteoblast Signaling
|
|
Focal Adhesion
|
|
PIP3 activates AKT signaling
|
|
Allograft Rejection
|
|
Signaling by PDGF
|
|
Bladder Cancer
|
|
Signaling by FGFRWP1919:Signaling by VEGFWP51:Regulation of Actin Cytoskeleton
|
|
PDGF Pathway
|
|
Signaling by PDGFWP306:Focal Adhesion
|
|
Angiogenesis
|
| References |
| REF 1 | 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. |
|---|
| REF 2 | (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). |
|---|
| REF 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. doi: 10.1158/0008-5472.CAN-10-2700. Epub 2011 Jan 6. |
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