Drug Information

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 [524749], [542632]
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
25031915
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 [525382]
Fibroblast growth factor receptor 2 Target Info Inhibitor [525382]
Vascular endothelial growth factor receptor 2 Target Info Inhibitor [525382]
Alpha platelet-derived growth factor receptor Target Info Inhibitor [525382]
FGF-3 receptor Target Info Inhibitor [525382]
Vascular endothelial growth factor receptor 3 Target Info Inhibitor [525382]
Beta platelet-derived growth factor receptor Target Info Inhibitor [525382]
Vascular endothelial growth factor receptor 1 Target Info Inhibitor [525382]
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 524749ClinicalTrials.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 542632(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 525382E-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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