drug_type
RELEVANT_DRUG
intervention_type
Small molecule kinase inhibitor
drug_description
Oral small-molecule HER2-selective tyrosine kinase inhibitor that blocks ERBB2 signaling (PI3K/AKT, MAPK) with CNS activity.
nci_thesaurus_concept_id
C77896
nci_thesaurus_preferred_term
Tucatinib
nci_thesaurus_definition
An orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity. Tucatinib selectively binds to and inhibits the phosphorylation of ErbB-2, which may prevent the activation of ErbB-2 signal transduction pathways, resulting in growth inhibition and death of ErbB-2-expressing tumor cells. ErbB-2 is overexpressed in a variety of cancers and plays an important role in cellular proliferation and differentiation.
drug_mesh_term
Tucatinib
drug_category
SMALL MOLECULE DRUG
drug_class
Inhibitor
drug_delivery_route
Oral
drug_mechanism_of_action
Oral HER2-selective tyrosine kinase inhibitor that binds the ERBB2 (HER2) intracellular kinase domain, blocks receptor phosphorylation and downstream PI3K/AKT and MAPK signaling, leading to inhibition of proliferation and death of HER2-overexpressing tumor cells; exhibits CNS penetration/activity.
drug_name
Tucatinib
nct_id_drug_ref
NCT04789096