NCI Drug Dictionary

The NCI Drug Dictionary contains technical definitions and synonyms for drugs/agents used to treat patients with cancer or conditions related to cancer. Each drug entry includes links to check for clinical trials listed in NCI's List of Cancer Clinical Trials.

osimertinib mesylate
Patient Information
The mesylate salt of an orally available, irreversible, third-generation, mutant-selective epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon oral administration, osimertinib mesylate selectively and covalently binds to and inhibits the activity of the mutant forms of EGFR, including the T790M EGFR mutant form, 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 overexpressed or mutated in many types of cancers, plays a key role in tumor cell proliferation and tumor vascularization. As osimertinib inhibits T790M, a secondarily acquired resistance mutation, this agent may have therapeutic benefits in tumors with T790M-mediated resistance. As this agent is selective towards mutant forms of EGFR, its toxicity profile may be reduced as compared to non-selective EGFR inhibitors, which also inhibit wild-type EGFR. Check for active clinical trials using this agent. (NCI Thesaurus)

Synonym:EGFR inhibitor AZD9291
US brand name:Tagrisso
Code name:AZD9291
Chemical structure:2-Propenamide, N-(2-((2-(dimethylamino)ethyl)methylamino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl)amino)phenyl)-