lapatinib

E902877

Lapatinib is an oral small-molecule tyrosine kinase inhibitor used primarily to treat HER2-positive breast cancer.

All labels observed (2)

Label Occurrences
lapatinib canonical 3
lapatinib ditosylate 1

How this entity was disambiguated

Statements (50)

Predicate Object
instanceOf EGFR inhibitor
HER2 inhibitor
antineoplastic agent
oral anticancer agent
protein kinase inhibitor
small-molecule drug
tyrosine kinase inhibitor
bindsTo ATP-binding site of EGFR
ATP-binding site of HER2
developedBy GlaxoSmithKline
hasApprovalBy European Medicines Agency
U.S. Food and Drug Administration
hasATCCode L01EB07
hasBioavailability low to moderate oral bioavailability
hasBoxedWarningFor hepatotoxicity
hasCASNumber 231277-92-2
hasChemicalFormula C29H26ClFN4O4S
hasCommonAdverseEffect diarrhea
fatigue
nausea
rash
hasEliminationHalfLife approximately 24 hours
hasMolecularWeight 581.06 g/mol
hasRouteOfAdministration oral
hasSeriousAdverseEffect cardiac dysfunction
hepatotoxicity
hasTradeName Tykerb
Tyverb
inhibits autophosphorylation of EGFR
autophosphorylation of HER2
isAdministeredAs lapatinib ditosylate
linked to: lapatinib
isHighlyProteinBound true
isMetabolizedBy CYP2C19
CYP2C8
CYP3A4
CYP3A5
isPregnancyCategory D (US, historical classification)
isSubstrateOf P-glycoprotein
mechanismOfAction reversible inhibition of HER2 and EGFR tyrosine kinases
oftenUsedWith capecitabine
linked to: Xeloda

letrozole
reduces downstream MAPK signaling
downstream PI3K/AKT signaling
targets EGFR
ERBB1
linked to: EGFR

ERBB2
HER2
linked to: ERBB2
usedFor HER2-positive breast cancer
advanced breast cancer
metastatic breast cancer

How these facts were elicited

Referenced by (4)

Full triples — surface form annotated when it differs from this entity's canonical label.

HER2 receptor targetOfDrug lapatinib
ERBB2 therapeuticTargetOf lapatinib
CD340 targetOf lapatinib
lapatinib isAdministeredAs lapatinib ditosylate
linked to: lapatinib