Afatinib
From Proteopedia
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Afatinib, sold under the brand name Gilotrif among others, is a medication which is used to 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]. | Afatinib, sold under the brand name Gilotrif among others, is a medication which is used to 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 | + | 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> |
| - | [[4g5j]]. | + | <scene name='10/1014269/Cv/3'>Epidermal growth factor receptor in complex with Afatinib</scene> ([[4g5j]]). |
</StructureSection> | </StructureSection> | ||
== References == | == References == | ||
<references/> | <references/> | ||
Revision as of 13:17, 14 December 2023
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References
- ↑ Spreitzer H (13 May 2008). "Neue Wirkstoffe – Tovok". Österreichische Apothekerzeitung (in German) (10/2008): 498.
- ↑ 2.0 2.1 Minkovsky N, Berezov A. BIBW-2992, a dual receptor tyrosine kinase inhibitor for the treatment of solid tumors. Curr Opin Investig Drugs. 2008 Dec;9(12):1336-46 PMID:19037840
- ↑ "Gilotrif (afatinib)" (PDF). US Food and Drug Administration. Retrieved 11 March 2021.
- ↑ "Giotrif Afatinib (as afatinib dimaleate)" (PDF). TGA eBusiness Services. Boehringer Ingelheim Pty Limited. 7 November 2013. Retrieved 28 January 2014.
- ↑ Li D, Ambrogio L, Shimamura T, Kubo S, Takahashi M, Chirieac LR, Padera RF, Shapiro GI, Baum A, Himmelsbach F, Rettig WJ, Meyerson M, Solca F, Greulich H, Wong KK. BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene. 2008 Aug 7;27(34):4702-11. PMID:18408761 doi:10.1038/onc.2008.109
