tucatinib
E902879
HER2 inhibitor
antineoplastic agent
approved drug
orally administered drug
protein kinase inhibitor
small-molecule tyrosine kinase inhibitor
Tucatinib is an oral small-molecule tyrosine kinase inhibitor used in the treatment of HER2-positive breast cancer, including cases with brain metastases.
Statements (49)
| Predicate | Object |
|---|---|
| instanceOf |
HER2 inhibitor
ⓘ
antineoplastic agent ⓘ approved drug ⓘ orally administered drug ⓘ protein kinase inhibitor ⓘ small-molecule tyrosine kinase inhibitor ⓘ |
| crosses | blood–brain barrier ⓘ |
| hasApprovalYear | 2020 ⓘ |
| hasATCCode | L01EH05 ⓘ |
| hasClinicalTrial | HER2CLIMB NERFINISHED ⓘ |
| hasCommonAdverseEffect |
diarrhea
ⓘ
elevated liver enzymes ⓘ fatigue ⓘ nausea ⓘ palmar-plantar erythrodysesthesia ⓘ vomiting ⓘ |
| hasDeveloper | Seagen Inc. NERFINISHED ⓘ |
| hasDosageForm | oral tablet ⓘ |
| hasEffect |
inhibits tumor cell proliferation in HER2-overexpressing cells
ⓘ
reduces phosphorylation of HER2 ⓘ reduces phosphorylation of downstream signaling proteins ⓘ |
| hasEffectInTrial |
improved overall survival in HER2-positive metastatic breast cancer
ⓘ
improved progression-free survival in HER2-positive metastatic breast cancer ⓘ |
| hasIndication |
HER2-positive breast cancer
ⓘ
HER2-positive breast cancer with brain metastases ⓘ HER2-positive metastatic colorectal cancer ⓘ metastatic HER2-positive breast cancer ⓘ unresectable HER2-positive breast cancer ⓘ |
| hasIndicationDetail | patients who have received prior anti-HER2-based regimens in the metastatic setting ⓘ |
| hasMechanismOfAction |
inhibition of HER2-driven cell signaling
ⓘ
selective inhibition of HER2 tyrosine kinase ⓘ |
| hasMolecularFormula | C26H24N8O2 ⓘ |
| hasMolecularWeight | 480.52 g/mol ⓘ |
| hasPregnancyCategory | embryo-fetal toxicity risk ⓘ |
| hasRouteOfAdministration | oral ⓘ |
| hasRouteOfElimination | hepatic ⓘ |
| hasSeriousAdverseEffect |
hepatotoxicity
ⓘ
severe diarrhea ⓘ |
| hasTradeName | Tukysa NERFINISHED ⓘ |
| hasUsualAdultDose | 300 mg twice daily ⓘ |
| isApprovedBy | U.S. Food and Drug Administration NERFINISHED ⓘ |
| isInhibitorOf |
CYP3A4
NERFINISHED
ⓘ
P-glycoprotein ⓘ |
| isMetabolizedBy |
CYP2C8
ⓘ
CYP3A4 ⓘ |
| isUsedInCombinationWith |
capecitabine
ⓘ
trastuzumab NERFINISHED ⓘ |
| targets |
ERBB2
NERFINISHED
ⓘ
HER2 NERFINISHED ⓘ |
Referenced by (2)
Full triples — surface form annotated when it differs from this entity's canonical label.