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drug_type
RELEVANT_DRUG
intervention_type
Drug
drug_description
A small-molecule, third-generation, irreversible EGFR tyrosine kinase inhibitor selective for mutant EGFR (including T790M), inhibiting EGFR signaling and downstream MAPK/ERK and PI3K/AKT pathways.
nci_thesaurus_concept_id
C116377
nci_thesaurus_preferred_term
Osimertinib
nci_thesaurus_definition
A third-generation, orally available, irreversible, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon oral administration, osimertinib covalently binds to and inhibits the activity of numerous mutant forms of EGFR, including the secondarily-acquired resistance mutation T790M, L858R, and exon 19 deletions, thereby preventing EGFR-mediated signaling. This may both induce cell death and inhibit tumor growth in EGFR-overexpressing tumor cells. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization. As this agent is selective towards mutant forms of EGFR, its toxicity profile may be reduced when compared to non-selective EGFR inhibitors which also inhibit wild-type EGFR.
drug_mesh_term
osimertinib
drug_category
SMALL MOLECULE DRUG
drug_class
Inhibitor
drug_delivery_route
Oral
drug_mechanism_of_action
Third-generation, irreversible, mutant-selective EGFR tyrosine kinase inhibitor that covalently binds EGFR (including T790M at Cys797), shutting down EGFR signaling and downstream MAPK/ERK and PI3K/AKT pathways to inhibit proliferation and induce tumor cell death.
drug_name
Osimertinib
nct_id_drug_ref
NCT05801029