lapatinib
E902877
EGFR inhibitor
HER2 inhibitor
antineoplastic agent
oral anticancer agent
protein kinase inhibitor
small-molecule drug
tyrosine kinase inhibitor
Lapatinib is an oral small-molecule tyrosine kinase inhibitor used primarily to treat HER2-positive breast cancer.
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 NERFINISHED ⓘ |
| hasApprovalBy |
European Medicines Agency
NERFINISHED
ⓘ
U.S. Food and Drug Administration NERFINISHED ⓘ |
| 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
NERFINISHED
ⓘ
Tyverb NERFINISHED ⓘ |
| inhibits |
autophosphorylation of EGFR
ⓘ
autophosphorylation of HER2 ⓘ |
| isAdministeredAs | lapatinib ditosylate NERFINISHED ⓘ |
| isHighlyProteinBound | true ⓘ |
| isMetabolizedBy |
CYP2C19
NERFINISHED
ⓘ
CYP2C8 NERFINISHED ⓘ CYP3A4 NERFINISHED ⓘ CYP3A5 NERFINISHED ⓘ |
| isPregnancyCategory | D (US, historical classification) ⓘ |
| isSubstrateOf | P-glycoprotein NERFINISHED ⓘ |
| mechanismOfAction | reversible inhibition of HER2 and EGFR tyrosine kinases ⓘ |
| oftenUsedWith |
capecitabine
NERFINISHED
ⓘ
letrozole ⓘ |
| reduces |
downstream MAPK signaling
ⓘ
downstream PI3K/AKT signaling ⓘ |
| targets |
EGFR
NERFINISHED
ⓘ
ERBB1 NERFINISHED ⓘ ERBB2 NERFINISHED ⓘ HER2 NERFINISHED ⓘ |
| usedFor |
HER2-positive breast cancer
ⓘ
advanced breast cancer ⓘ metastatic breast cancer ⓘ |
Referenced by (2)
Full triples — surface form annotated when it differs from this entity's canonical label.