drug_type
RELEVANT_DRUG
intervention_type
Drug
drug_description
Third-generation, mutant-selective, irreversible EGFR tyrosine kinase inhibitor.
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, mutant-selective, irreversible EGFR tyrosine kinase inhibitor that covalently binds mutant EGFR (e.g., T790M, L858R, exon 19 deletions), suppressing EGFR signaling to inhibit proliferation and induce apoptosis, with relatively reduced activity on wild-type EGFR.
drug_name
Osimertinib
nct_id_drug_ref
NCT06532149