| Drug General Information |
| Drug ID |
D07POC
|
| Former ID |
DAP001010
|
| Drug Name |
Erlotinib
|
| Synonyms |
Erlotinin; Tarceva; Erlotinib Base; AQ4; OSI 744; R 1415; CP 358,774; CP-358774; Erlotinib(Tarceva); Tarceva (TN); CP-358,774; Erlotinib, OS-774; N-(3-ethynylphenyl)[6,7-bis(2-methoxyethoxy)quinazolin-4-yl]amine; N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine; N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine; N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-Quinazolinamine; [6,7-BIS(2-METHOXY-ETHOXY)QUINAZOLINE-4-YL]-(3-ETHYNYLPHENYL)AMINE; [6,7-Bis-(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)-amine; 4-[(3-Ethynylphenyl)amino]-6,7-bis(2-methoxyethoxy)quinazoline; 4-[(3-ethynylphenyl)amino]-6,7-bis(2-methoxyethoxy)quinazoline; Tyrosine Kinase Inhibitor - Ns
|
| Drug Type |
Small molecular drug
|
| Indication |
Non-small cell lung cancer [ICD10:C33-C34]
|
Approved |
[1],
[2]
|
|---|
|
Pancreatic cancer [ICD9: 140-199, 140-229, 157, 210-229; ICD10:C25]
|
Phase 3 |
[1],
[3]
|
|
Colon cancer; Glioma; Breast cancer; Head and neck cancer [ICD9: 140-149, 140-229, 183, 191; ICD10:C00-C96, C07-C14, C32, C33, C56, C71]
|
Phase 2 |
[1],
[3]
|
| Therapeutic Class |
Anticancer Agents
|
| Company |
OSI Pharma
|
| Structure |
|
Download
2D MOL
3D MOL
|
| Formula |
C22H23N3O4
|
| InChI |
InChI=1S/C22H23N3O4/c1-4-16-6-5-7-17(12-16)25-22-18-13-20(28-10-8-26-2)21(29-11-9-27-3)14-19(18)23-15-24-22/h1,5-7,12-15H,8-11H2,2-3H3,(H,23,24,25)
|
| InChIKey |
AAKJLRGGTJKAMG-UHFFFAOYSA-N
|
| CAS Number |
CAS 183321-74-6
|
| PubChem Compound ID |
|
| PubChem Substance ID |
826174, 6593089, 7885946, 8035065, 10258448, 14720343, 14878691, 21317842, 26757996, 33500421, 46508021, 47957324, 50068213, 50100099, 50405936, 53788276, 57395323, 68530774, 85171065, 85261833, 85267493, 87350514, 92308781, 92717787, 93581027, 94568883, 103177459, 103905339, 104425943, 104831334, 117695448, 117866919, 118049695, 124893165, 124893166, 125001915, 125343507, 126622002, 126653679, 126670959, 126670960, 127301426, 127301427, 127301428, 127301429, 127301430, 127301431, 127301432, 127301433, 127301434
|
| SuperDrug ATC ID |
L01XE03
|
| Drug Resistance Mutation (DRM) |
| DRM |
DRM Info
|
| Target and Pathway |
| Target(s) |
Epidermal growth factor receptor |
Target Info |
Inhibitor |
[4]
|
|---|
|
KEGG Pathway
|
MAPK signaling pathway
|
|
ErbB signaling pathway
|
|
Ras signaling pathway
|
|
Rap1 signaling pathway
|
|
Calcium signaling pathway
|
|
Cytokine-cytokine receptor interaction
|
|
HIF-1 signaling pathway
|
|
FoxO signaling pathway
|
|
Endocytosis
|
|
PI3K-Akt signaling pathway
|
|
Dorso-ventral axis formation
|
|
Focal adhesion
|
|
Adherens junction
|
|
Gap junction
|
|
Regulation of actin cytoskeleton
|
|
GnRH signaling pathway
|
|
Estrogen signaling pathway
|
|
Oxytocin signaling pathway
|
|
Epithelial cell signaling in Helicobacter pylori infection
|
|
Hepatitis C
|
|
Pathways in cancer
|
|
Proteoglycans in cancer
|
|
MicroRNAs in cancer
|
|
Pancreatic cancer
|
|
Endometrial cancer
|
|
Glioma
|
|
Prostate cancer
|
|
Melanoma
|
|
Bladder cancer
|
|
Non-small cell lung cancer
|
|
Central carbon metabolism in cancer
|
|
Choline metabolism in cancer
|
|
NetPath Pathway
|
IL4 Signaling Pathway
|
|
EGFR1 Signaling Pathway
|
|
PANTHER Pathway
|
Cadherin signaling pathway
|
|
EGF receptor signaling pathway
|
|
Pathway Interaction Database
|
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
|
|
ErbB receptor signaling network
|
|
Internalization of ErbB1
|
|
Stabilization and expansion of the E-cadherin adherens junction
|
|
a6b1 and a6b4 Integrin signaling
|
|
Syndecan-3-mediated signaling events
|
|
Reactome
|
Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants
|
|
SHC1 events in ERBB2 signaling
|
|
PLCG1 events in ERBB2 signaling
|
|
PIP3 activates AKT signaling
|
|
GRB2 events in EGFR signaling
|
|
GAB1 signalosome
|
|
SHC1 events in EGFR signaling
|
|
EGFR downregulation
|
|
GRB2 events in ERBB2 signaling
|
|
PI3K events in ERBB2 signaling
|
|
EGFR Transactivation by Gastrin
|
|
Constitutive Signaling by Aberrant PI3K in Cancer
|
|
Constitutive Signaling by EGFRvIII
|
|
RAF/MAP kinase cascade
|
|
WikiPathways
|
ErbB Signaling Pathway
|
|
Regulation of Actin Cytoskeleton
|
|
EGF/EGFR Signaling Pathway
|
|
MAPK Signaling Pathway
|
|
Focal Adhesion
|
|
Aryl Hydrocarbon Receptor Pathway
|
|
Extracellular vesicle-mediated signaling in recipient cells
|
|
TCA Cycle Nutrient Utilization and Invasiveness of Ovarian Cancer
|
|
Hair Follicle Development: Cytodifferentiation (Part 3 of 3)
|
|
Bladder Cancer
|
|
Hair Follicle Development: Induction (Part 1 of 3)
|
|
Signaling by ERBB4
|
|
Signaling by ERBB2
|
|
Gastrin-CREB signalling pathway via PKC and MAPK
|
|
PIP3 activates AKT signaling
|
|
Nanoparticle-mediated activation of receptor signaling
|
|
Aryl Hydrocarbon Receptor
|
|
Spinal Cord Injury
|
|
Integrated Pancreatic Cancer Pathway
|
|
Gastric cancer network 2
|
|
AGE/RAGE pathway
|
|
Signaling Pathways in Glioblastoma
|
|
Arylhydrocarbon receptor (AhR) signaling pathway
|
|
miR-targeted genes in muscle cell - TarBase
|
|
miR-targeted genes in lymphocytes - TarBase
|
|
miR-targeted genes in epithelium - TarBase
|
|
Integrated Breast Cancer Pathway
|
|
Signaling by EGFR
|
|
L1CAM interactions
|
| References |
| REF 1 | (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: 4920). |
|---|
| REF 2 | 2004 approvals: the demise of the blockbuster. Nat Rev Drug Discov. 2005 Feb;4(2):93-4. |
|---|
| REF 3 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. |
|---|
| REF 4 | Quantitative Prediction of Fold Resistance for Inhibitors of EGFR. Biochemistry. 2009 Jul 23. |
|---|
