| Drug General Information |
| Drug ID |
D09XZB
|
| Former ID |
DAP000657
|
| Drug Name |
Gefitinib
|
| Synonyms |
Gefitini; IRE; Iressa; Irressat; Gefitinib [USAN]; ZD 1839; ZD1839; Iressa (TN); Iressa(TM); ZD-1839; CU-00000000396-1; Gefitinib,Iressa, ZD1839; Gefitinib (JAN/USAN/INN); ZD-1839, Iressa, Gefitinib; N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-amine; N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-(4-morpholinyl)propoxy)-4-quinazolinamide; N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine; N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(morpholin-4-yl)propoxy]quinazolin-4-amine; N-(3-Chloro-4-fluoro-phenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine; 4-(3'-Chloro-4'-fluoroanilino)-7-methoxy-6-(3-morpholinopropoxy)quinazoline; 6-(3-morpholinopropoxy)-N-(3-chloro-4-fluorophenyl)-7-methoxyquinazolin-4-amine; Tyrosine Kinase Inhibitor - Ns
|
| Drug Type |
Small molecular drug
|
| Indication |
Cancer [ICD9: 140-229; ICD10:C00-C96]
|
Approved |
[1],
[2]
|
|---|
|
Head and neck cancer [ICD9: 140-149, 140-229; ICD10:C07-C14, C32-C33]
|
Phase 3 |
[1],
[2]
|
|
Urethral cancer; Bladder cancer; Ovarian cancer; Prostate cancer; Breast cancer [ICD9: 140-229, 174, 175, 183, 188; ICD10:C50, C56, C67]
|
Phase 2 |
[1],
[2]
|
| Therapeutic Class |
Anticancer Agents
|
| Company |
AstraZeneca
|
| Structure |
|
Download
2D MOL
3D MOL
|
| Formula |
C22H24ClFN4O3
|
| InChI |
InChI=1S/C22H24ClFN4O3/c1-29-20-13-19-16(12-21(20)31-8-2-5-28-6-9-30-10-7-28)22(26-14-25-19)27-15-3-4-18(24)17(23)11-15/h3-4,11-14H,2,5-10H2,1H3,(H,25,26,27)
|
| InChIKey |
XGALLCVXEZPNRQ-UHFFFAOYSA-N
|
| CAS Number |
CAS 184475-35-2
|
| PubChem Compound ID |
|
| PubChem Substance ID |
532631, 7849039, 8035066, 10240807, 10318995, 11377941, 12015033, 14833109, 21317853, 24424016, 24424024, 24424026, 29215403, 29215404, 29303859, 46508649, 47646567, 49635529, 49742641, 50040863, 50100103, 53319998, 53788589, 53799235, 56312091, 56313236, 56313469, 57340492, 61127928, 81092810, 85171051, 92308715, 92717784, 93581024, 99436946, 99444469, 103024897, 103244983, 103905343, 103905344, 104418951, 104829175, 117865087, 118047033, 123105108, 124756943, 124892204, 124892205, 124892206, 125001914
|
| ChEBI ID |
ChEBI:49668
|
| SuperDrug ATC ID |
L01XE02
|
| SuperDrug CAS ID |
cas=184475352
|
| Drug Resistance Mutation (DRM) |
| DRM |
DRM Info
|
| Target and Pathway |
| Target(s) |
Epidermal growth factor receptor |
Target Info |
Inhibitor |
[3],
[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: 4941). |
|---|
| REF 2 | Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91. |
|---|
| REF 3 | Targeting' the epidermal growth factor receptor tyrosine kinase with gefitinib (Iressa) in non-small cell lung cancer (NSCLC). Semin Cancer Biol. 2004 Feb;14(1):33-40. |
|---|
| REF 4 | Gefitinib ('Iressa', ZD1839) and new epidermal growth factor receptor inhibitors. Br J Cancer. 2004 Feb 9;90(3):566-72. |
|---|
