| Drug General Information |
| Drug ID |
D05UFG
|
| Former ID |
DCL000498
|
| Drug Name |
BIBW 2992
|
| Synonyms |
Afatinib; Tomtovok; Tovok; BIBW-2992; Tovok (TN); Tovok, BIBW2992; (2E)-N-{4-[(3-chloro-4-fluorophenyl)amino]-7-[(3S)-tetrahydrofuran-3-yloxy]quinazolin-6-yl}-4-(dimethylamino)but-2-enamide; EGFR inhibitor 2nd gens
|
| Drug Type |
Small molecular drug
|
| Indication |
Non-small cell lung cancer [ICD10:C33-C34]
|
Approved |
[1],
[2]
|
|---|
| Company |
Boehringer Ingelheim
|
| Structure |
|
Download
2D MOL
3D MOL
|
| Formula |
C24H25ClFN5O3
|
| InChI |
InChI=1S/C24H25ClFN5O3/c1-31(2)8-3-4-23(32)30-21-11-17-20(12-22(21)34-16-7-9-33-13-16)27-14-28-24(17)29-15-5-6-19(26)18(25)10-15/h3-6,10-12,14,16H,7-9,13H2,1-2H3,(H,30,32)(H,27,28,29)/b4-3+/t16-/m0/s1
|
| InChIKey |
ULXXDDBFHOBEHA-CWDCEQMOSA-N
|
| CAS Number |
CAS 850140-72-6
|
| PubChem Compound ID |
|
| PubChem Substance ID |
15180141, 22579524, 40274223, 57304398, 78996079, 99432363, 103768626, 104144352, 111978343, 118049494, 123051125, 124490464, 124756933, 124896577, 125163740, 125329929, 126578844, 126666994, 126726460, 131407778, 131465104, 134222879, 134339089, 135257273, 135267496, 135727456, 136368046, 136920296, 137039955, 137263401, 142681900, 143499145, 144072463, 144115710, 151990100, 152043638, 152234944, 152258159, 152344140, 160646996, 162011458, 162037384, 162202549, 163404060, 163406016, 164041641, 164825245, 164835145, 165245589, 170502166
|
| SuperDrug ATC ID |
L01XE13
|
| Drug Resistance Mutation (DRM) |
| DRM |
DRM Info
|
| Target and Pathway |
| Target(s) |
Receptor protein-tyrosine kinase erbB-2 |
Target Info |
Inhibitor |
[3]
|
|---|
| Epidermal growth factor receptor |
Target Info |
Inhibitor |
[3]
|
|
KEGG Pathway
|
ErbB signaling pathway
|
|
Calcium signaling pathway
|
|
HIF-1 signaling pathway
|
|
Focal adhesion
|
|
Adherens junction
|
|
Pathways in cancer
|
|
Proteoglycans in cancer
|
|
MicroRNAs in cancer
|
|
Pancreatic cancer
|
|
Endometrial cancer
|
|
Prostate cancer
|
|
Bladder cancer
|
|
Non-small cell lung cancer
|
|
Central carbon metabolism in cancerhsa04010:MAPK signaling pathway
|
|
Ras signaling pathway
|
|
Rap1 signaling pathway
|
|
Cytokine-cytokine receptor interaction
|
|
FoxO signaling pathway
|
|
Endocytosis
|
|
PI3K-Akt signaling pathway
|
|
Dorso-ventral axis formation
|
|
Gap junction
|
|
Regulation of actin cytoskeleton
|
|
GnRH signaling pathway
|
|
Estrogen signaling pathway
|
|
Oxytocin signaling pathway
|
|
Epithelial cell signaling in Helicobacter pylori infection
|
|
Hepatitis C
|
|
Glioma
|
|
Melanoma
|
|
Central carbon metabolism in cancer
|
|
Choline metabolism in cancer
|
|
NetPath Pathway
|
TCR Signaling PathwayNetPath_16:IL4 Signaling Pathway
|
|
EGFR1 Signaling Pathway
|
|
PANTHER Pathway
|
Cadherin signaling pathway
|
|
EGF receptor signaling pathwayP00012:Cadherin signaling pathway
|
|
EGF receptor signaling pathway
|
|
Pathway Interaction Database
|
ErbB4 signaling events
|
|
ErbB2/ErbB3 signaling events
|
|
ErbB receptor signaling network
|
|
a6b1 and a6b4 Integrin signaling
|
|
Validated targets of C-MYC transcriptional repressionlysophospholipid_pathway:LPA receptor mediated events
|
|
Signaling events mediated by PTP1B
|
|
Arf6 signaling events
|
|
Signaling events mediated by TCPTP
|
|
Thromboxane A2 receptor signaling
|
|
SHP2 signaling
|
|
Regulation of Telomerase
|
|
EGF receptor (ErbB1) signaling pathway
|
|
EGFR-dependent Endothelin signaling events
|
|
Posttranslational regulation of adherens junction stability and dissassembly
|
|
Direct p53 effectors
|
|
ErbB1 downstream signaling
|
|
Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling
|
|
E-cadherin signaling in keratinocytes
|
|
Internalization of ErbB1
|
|
Stabilization and expansion of the E-cadherin adherens junction
|
|
Syndecan-3-mediated signaling events
|
|
PathWhiz Pathway
|
Phosphatidylinositol Phosphate Metabolism
|
|
Reactome
|
SHC1 events in ERBB2 signaling
|
|
PLCG1 events in ERBB2 signaling
|
|
PIP3 activates AKT signaling
|
|
GRB2 events in ERBB2 signaling
|
|
PI3K events in ERBB2 signaling
|
|
Constitutive Signaling by Aberrant PI3K in Cancer
|
|
Sema4D induced cell migration and growth-cone collapse
|
|
RAF/MAP kinase cascadeR-HSA-1236382:Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants
|
|
GRB2 events in EGFR signaling
|
|
GAB1 signalosome
|
|
SHC1 events in EGFR signaling
|
|
EGFR downregulation
|
|
EGFR Transactivation by Gastrin
|
|
Constitutive Signaling by EGFRvIII
|
|
RAF/MAP kinase cascade
|
|
WikiPathways
|
DNA Damage Response (only ATM dependent)
|
|
ErbB Signaling Pathway
|
|
EGF/EGFR Signaling Pathway
|
|
Focal Adhesion
|
|
Extracellular vesicle-mediated signaling in recipient cells
|
|
Bladder Cancer
|
|
Signaling by ERBB2
|
|
Integrated Pancreatic Cancer Pathway
|
|
Signaling Pathways in Glioblastoma
|
|
Leptin signaling pathway
|
|
miR-targeted genes in muscle cell - TarBase
|
|
Semaphorin interactionsWP673:ErbB Signaling Pathway
|
|
Regulation of Actin Cytoskeleton
|
|
MAPK Signaling Pathway
|
|
Aryl Hydrocarbon Receptor Pathway
|
|
TCA Cycle Nutrient Utilization and Invasiveness of Ovarian Cancer
|
|
Hair Follicle Development: Cytodifferentiation (Part 3 of 3)
|
|
Hair Follicle Development: Induction (Part 1 of 3)
|
|
Signaling by ERBB4
|
|
Gastrin-CREB signalling pathway via PKC and MAPK
|
|
PIP3 activates AKT signaling
|
|
Nanoparticle-mediated activation of receptor signaling
|
|
Aryl Hydrocarbon Receptor
|
|
Spinal Cord Injury
|
|
Gastric cancer network 2
|
|
AGE/RAGE pathway
|
|
Arylhydrocarbon receptor (AhR) signaling pathway
|
|
miR-targeted genes in lymphocytes - TarBase
|
|
miR-targeted genes in epithelium - TarBase
|
|
Integrated Breast Cancer Pathway
|
|
Signaling by EGFR
|
|
L1CAM interactions
|
| References |
| REF 1 | BIBW-2992, a dual receptor tyrosine kinase inhibitor for the treatment of solid tumors. Curr Opin Investig Drugs. 2008 Dec;9(12):1336-46. |
|---|
| 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: 5667). |
|---|
| REF 3 | Boehringer Ingelheim. Product Development Pipeline. June 2 2009. |
|---|
