View source for Afatinib

<StructureSection load='' size='340' side='right' caption='Afatinib' scene='10/1014269/Cv/1'>
Afatinib, sold under the brand name Gilotrif among others, is a medication which is used to [[Treatment non-small cell lung carcinoma|treat non-small cell lung carcinoma]] (NSCLC).<ref name="a2">Spreitzer H (13 May 2008). "Neue Wirkstoffe – Tovok". Österreichische Apothekerzeitung (in German) (10/2008): 498.</ref><ref name="a3">PMID:19037840</ref><ref name="a4">[https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/201292s014lbl.pdf "Gilotrif (afatinib)"] (PDF). US Food and Drug Administration. Retrieved 11 March 2021.</ref> It belongs to the tyrosine kinase inhibitor family of medications.<ref name="a5">[https://www.ebs.tga.gov.au/ebs/picmi/picmirepository.nsf/pdf?OpenAgent&id=CP-2013-PI-02417-1 "Giotrif Afatinib (as afatinib dimaleate)"] (PDF). TGA eBusiness Services. Boehringer Ingelheim Pty Limited. 7 November 2013. Retrieved 28 January 2014.</ref> See also [https://en.wikipedia.org/wiki/Afatinib Afatinib].

Like [[lapatinib]] and neratinib, afatinib is a protein kinase inhibitor that also irreversibly inhibits human epidermal growth factor receptor 2 ([[Herceptin - Mechanism of Action|Her2]]) and [[epidermal growth factor receptor]] (EGFR) kinases. Afatinib is not only active against EGFR mutations targeted by first generation [[Tyrosine Kinase Inhibitor Pharmacokinetics|tyrosine-kinase inhibitors]] (TKIs) like [[erlotinib]] or [[gefitinib]], but also against less common mutations which are resistant to these drugs. However, it is not active against the T790M mutation which generally requires third generation drugs like [[osimertinib]].<ref name="a12">PMID:18408761</ref> Because of its additional activity against Her2, it is being investigated for breast cancer as well as other EGFR and Her2 driven cancers.<ref name="a3">PMID:19037840</ref>

<scene name='10/1014269/Cv/3'>Epidermal growth factor receptor in complex with Afatinib</scene> ([[4g5j]]).

<scene name='10/1014269/Cv/4'>Afatinib binding site</scene>.

<scene name='10/1014269/Cv/5'>Afatinib covalently binds to cysteine number 797</scene> of the epidermal growth factor receptor via a Michael addition (IC<sub>50</sub> = 0.5 nM).<ref name="a13">Schubert-Zsilavecz, M, Wurglics, M, Neue Arzneimittel Frühjahr 2013. (in German)</ref>

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== References ==
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