Afatinib: Difference between revisions
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<StructureSection load='' size='340' side='right' caption=' | <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 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 [[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 | 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]]). | ||
<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> | |||
</StructureSection> | </StructureSection> | ||
== References == | == References == | ||
<references/> | <references/> | ||
Latest revision as of 16:16, 15 February 2024
Afatinib, sold under the brand name Gilotrif among others, is a medication which is used to treat non-small cell lung carcinoma (NSCLC).[1][2][3] It belongs to the tyrosine kinase inhibitor family of medications.[4] See also Afatinib. Like lapatinib and neratinib, afatinib is a protein kinase inhibitor that also irreversibly inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases. Afatinib is not only active against EGFR mutations targeted by first generation 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.[5] Because of its additional activity against Her2, it is being investigated for breast cancer as well as other EGFR and Her2 driven cancers.[2] (4g5j). . of the epidermal growth factor receptor via a Michael addition (IC50 = 0.5 nM).[6]
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ReferencesReferences
- ↑ 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
- ↑ Schubert-Zsilavecz, M, Wurglics, M, Neue Arzneimittel Frühjahr 2013. (in German)