Ac0010ma - the maleate salt form of avitinib, an orally available, irreversible, epidermal growth factor receptor (egfr) mutant-selective inhibitor, with potential antineoplastic activity. Upon oral administration, avitinib covalently binds to and inhibits the activity of mutant forms of egfr, including the drug-resistant t790m egfr mutant, which prevents signaling mediated by mutant forms of egfr. This may both induce cell death and inhibit tumor growth in egfr-mutated tumor cells. Egfr, a receptor tyrosine kinase that is mutated in a variety of cancers, 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.
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