| Drug General Information |
| Drug ID |
D08CDI
|
| Former ID |
DAP000853
|
| Drug Name |
Lapatinib
|
| Synonyms |
FMM; Tycerb; Lapatinib Ditosylate; Lapatinib [INN]; Lapatinib tosilate hydrate; GSK 572016; GSK572016; GW 572016; GW 572016X; GW572016; Lapatinib (INN); Tykerb (TN); Lapatinib, Tykerb, GW572016; N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]furan-2-yl]quinazolin-4-amine; N-{3-CHLORO-4-[(3-FLUOROBENZYL)OXY]PHENYL}-6-[5-({[2-(METHYLSULFONYL)ETHYL]AMINO}METHYL)-2-FURYL]-4-QUINAZOLINAMINE; N-(3-Chloro-4-((3-fluorophenyl)methoxy)phenyl)-6-(5-((2-methylsulfonylethylamino)methyl)-2-furyl)quinazolin-4-amine; N-(3-Chloro-4-{[(3-fluorophenyl)methyl]oxy}phenyl)-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furanyl]-4-quinazolinamine; 4-[[3-Chloro-4-(3-fluorobenzyloxy)phenyl]amino]-6-[5-[[(2-methanesulfonylethyl)amino]methyl]furan-2-yl]quinazoline; Lapatinib (ERBB2 inhibitor)
|
| Drug Type |
Small molecular drug
|
| Indication |
Breast cancer [ICD9: 174, 175; ICD10:C50]
|
Approved |
[1],
[2]
|
|---|
| Therapeutic Class |
Anticancer Agents
|
| Company |
GlaxoSmithKline
|
| Structure |
|
Download
2D MOL
3D MOL
|
| Formula |
C29H26ClFN4O4S
|
| InChI |
InChI=1S/C29H26ClFN4O4S/c1-40(36,37)12-11-32-16-23-7-10-27(39-23)20-5-8-26-24(14-20)29(34-18-33-26)35-22-6-9-28(25(30)15-22)38-17-19-3-2-4-21(31)13-19/h2-10,13-15,18,32H,11-12,16-17H2,1H3,(H,33,34,35)
|
| InChIKey |
BCFGMOOMADDAQU-UHFFFAOYSA-N
|
| CAS Number |
CAS 388082-78-8
|
| PubChem Compound ID |
|
| PubChem Substance ID |
585695, 7887520, 8035064, 9368726, 14911387, 21317859, 30413551, 46393564, 46506302, 46507141, 49742619, 50070568, 50071307, 50100107, 50112760, 50644701, 53788364, 57399558, 85171071, 85202079, 91147938, 92308826, 92719029, 93581028, 96024798, 103177479, 103854383, 103905567, 103905568, 109692966, 113442073, 117695459, 124360113, 124893335, 124893336, 125345521, 126592984, 126621155, 126649062, 126666978, 126667073, 126731332, 127325943, 127325944, 127325945, 127494626, 134338132, 135128225, 135685383, 135685387
|
| SuperDrug ATC ID |
L01XE07
|
| Drug Resistance Mutation (DRM) |
| DRM |
DRM Info
|
| Target and Pathway |
| Target(s) |
Epidermal growth factor receptor |
Target Info |
Inhibitor |
[3],
[4]
|
|---|
| Receptor protein-tyrosine kinase erbB-2 |
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 cancerhsa04012:ErbB signaling pathway
|
|
NetPath Pathway
|
IL4 Signaling Pathway
|
|
EGFR1 Signaling PathwayNetPath_11:TCR Signaling Pathway
|
|
PANTHER Pathway
|
Cadherin signaling pathway
|
|
EGF receptor signaling pathwayP00012: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 eventserbb4_pathway:ErbB4 signaling events
|
|
ErbB2/ErbB3 signaling events
|
|
Validated targets of C-MYC transcriptional repression
|
|
PathWhiz Pathway
|
Phosphatidylinositol Phosphate Metabolism
|
|
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 cascadeR-HSA-1250196:SHC1 events in ERBB2 signaling
|
|
Sema4D induced cell migration and growth-cone collapse
|
|
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 interactionsWP710:DNA Damage Response (only ATM dependent)
|
|
Leptin signaling pathway
|
|
Semaphorin interactions
|
| References |
| REF 1 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 022059. |
|---|
| 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: 5692). |
|---|
| REF 3 | Multi-target therapeutics: when the whole is greater than the sum of the parts. Drug Discov Today. 2007 Jan;12(1-2):34-42. Epub 2006 Nov 28. |
|---|
| REF 4 | Triple negative breast cancer--current status and prospective targeted treatment based on HER1 (EGFR), TOP2A and C-MYC gene assessment. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2009 Mar;153(1):13-7. |
|---|
