NCI Drug Dictionary
The search textbox has an autosuggest feature. When you enter three or more characters, a list of up to 10 suggestions will popup under the textbox. Use the arrow keys to move through the suggestions. To select a suggestion, hit the enter key. Using the escape key closes the listbox and puts you back at the textbox. The radio buttons allow you to toggle between having all search items start with or contain the text you entered in the search box.
The dimaleate salt form of afatinib, an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity. Upon administration, afatinib selectively and irreversibly binds to and inhibits the epidermal growth factor receptors 1 (ErbB1; EGFR), 2 (ErbB2; HER2), and 4 (ErbB4; HER4), and certain EGFR mutants, including those caused by EGFR exon 19 deletion mutations or exon 21 (L858R) mutations. This may result in the inhibition of tumor growth and angiogenesis in tumor cells overexpressing these RTKs. Additionally, afatinib inhibits the EGFR T790M gatekeeper mutation which is resistant to treatment with first-generation EGFR inhibitors. EGFR, HER2 and HER4 are RTKs that belong to the EGFR superfamily; they play major roles in both tumor cell proliferation and tumor vascularization and are overexpressed in many cancer cell types. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)
|US brand name:||Gilotrif|
|Code name:||BIBW 2992 MA2|
|Chemical structures:||(2E)-N-(4-((3-chloro-4-fluorophenyl)amino)-7-(((3S)-tetrahydrofuran-3-yl)oxy)quinazolin- 6-yl)-4-(dimethylamino)but-2-enamide bis(hydrogen (2Z)-but-2-enedioate) |
2-butenamide, N-(4-((3-chloro-4-fluorophenyl)amino)-7-(((3S)-tetrahydro-3-furanyl)oxy)- 6-quinazolinyl)-4-(dimethylamino)-, (2E)-, (2Z)-2-butenedioate (1:2)