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Epidermal growth factor receptor inhibitors (view source)
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'''Epidermal growth factor receptor inhibitors''', abbreviated '''EGFR inhibitors''', is a class of drugs that blocks the EGF receptor. | '''Epidermal growth factor receptor inhibitors''', abbreviated '''EGFR inhibitors''', is a class of drugs that blocks the EGF receptor. | ||
==EGFR== | |||
*EGFR (aka. ErbB1 or HER1) is a membranous receptor expressed in epithelial cells. | |||
*Most of activating mutations in [[NSCLC]] are in Exon 18-21 (kinase domain). | |||
*45% of the mutations are p.DEL19, approx 40-45% are p.L858R, approx 2% are p.T790M. | |||
==Drugs== | ==Drugs== | ||
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*[[Gefitinib]] (''Iressa'', AstraZeneca).<ref name=pmid20855837/> | *[[Gefitinib]] (''Iressa'', AstraZeneca).<ref name=pmid20855837/> | ||
*[[Erlotinib]] (''Tarceva'', Roche).<ref name=pmid20855837>{{cite journal |author=Sun Y, Ren Y, Fang Z, ''et al.'' |title=Lung adenocarcinoma from East Asian never-smokers is a disease largely defined by targetable oncogenic mutant kinases |journal=J. Clin. Oncol. |volume=28 |issue=30 |pages=4616–20 |year=2010 |month=October |pmid=20855837 |doi=10.1200/JCO.2010.29.6038 |url=}}</ref> | *[[Erlotinib]] (''Tarceva'', Roche).<ref name=pmid20855837>{{cite journal |author=Sun Y, Ren Y, Fang Z, ''et al.'' |title=Lung adenocarcinoma from East Asian never-smokers is a disease largely defined by targetable oncogenic mutant kinases |journal=J. Clin. Oncol. |volume=28 |issue=30 |pages=4616–20 |year=2010 |month=October |pmid=20855837 |doi=10.1200/JCO.2010.29.6038 |url=}}</ref> | ||
Second generation: | Second generation: | ||
*Dacomitinib (''Vizimpro'', Pfizer) - not effective when EGFR T790M mutation present.<ref>{{Cite journal | last1 = Mok | first1 = TS. | last2 = Cheng | first2 = Y. | last3 = Zhou | first3 = X. | last4 = Lee | first4 = KH. | last5 = Nakagawa | first5 = K. | last6 = Niho | first6 = S. | last7 = Lee | first7 = M. | last8 = Linke | first8 = R. | last9 = Rosell | first9 = R. | title = Improvement in Overall Survival in a Randomized Study That Compared Dacomitinib With Gefitinib in Patients With Advanced Non-Small-Cell Lung Cancer and EGFR-Activating Mutations. | journal = J Clin Oncol | volume = | issue = | pages = JCO2018787994 | month = Jun | year = 2018 | doi = 10.1200/JCO.2018.78.7994 | PMID = 29864379 }}</ref> | *Dacomitinib (''Vizimpro'', Pfizer) - not effective when EGFR T790M mutation present.<ref>{{Cite journal | last1 = Mok | first1 = TS. | last2 = Cheng | first2 = Y. | last3 = Zhou | first3 = X. | last4 = Lee | first4 = KH. | last5 = Nakagawa | first5 = K. | last6 = Niho | first6 = S. | last7 = Lee | first7 = M. | last8 = Linke | first8 = R. | last9 = Rosell | first9 = R. | title = Improvement in Overall Survival in a Randomized Study That Compared Dacomitinib With Gefitinib in Patients With Advanced Non-Small-Cell Lung Cancer and EGFR-Activating Mutations. | journal = J Clin Oncol | volume = | issue = | pages = JCO2018787994 | month = Jun | year = 2018 | doi = 10.1200/JCO.2018.78.7994 | PMID = 29864379 }}</ref> | ||
*Afatinib (Gilotrif) - esp. effective when del19 is present.<ref>{{Cite journal | last1 = Yang | first1 = JC. | last2 = Wu | first2 = YL. | last3 = Schuler | first3 = M. | last4 = Sebastian | first4 = M. | last5 = Popat | first5 = S. | last6 = Yamamoto | first6 = N. | last7 = Zhou | first7 = C. | last8 = Hu | first8 = CP. | last9 = O'Byrne | first9 = K. | title = Afatinib versus cisplatin-based chemotherapy for EGFR mutation-positive lung adenocarcinoma (LUX-Lung 3 and LUX-Lung 6): analysis of overall survival data from two randomised, phase 3 trials. | journal = Lancet Oncol | volume = 16 | issue = 2 | pages = 141-51 | month = Feb | year = 2015 | doi = 10.1016/S1470-2045(14)71173-8 | PMID = 25589191 }}</ref> | |||
Third generation: | |||
*Osimertinib <ref>{{Cite journal | last1 = Alsharedi | first1 = M. | last2 = Bukamur | first2 = H. | last3 = Elhamdani | first3 = A. | title = Osimertinib for the treatment of patients with | journal = Drugs Today (Barc) | volume = 54 | issue = 6 | pages = 369-379 | month = Jun | year = 2018 | doi = 10.1358/dot.2018.54.6.2817668 | PMID = 29998228 }}</ref> | *Osimertinib <ref>{{Cite journal | last1 = Alsharedi | first1 = M. | last2 = Bukamur | first2 = H. | last3 = Elhamdani | first3 = A. | title = Osimertinib for the treatment of patients with | journal = Drugs Today (Barc) | volume = 54 | issue = 6 | pages = 369-379 | month = Jun | year = 2018 | doi = 10.1358/dot.2018.54.6.2817668 | PMID = 29998228 }}</ref> | ||
*Nazartinib | |||
Note: | Note: | ||
*Both ''gefitinib'' and ''erlotinib'' are also classified as ''[[tyrosine kinase inhibitors]]'' (TKIs). | *Both ''gefitinib'' and ''erlotinib'' are also classified as ''[[tyrosine kinase inhibitors]]'' (TKIs). After 10-12 months, tumors usu. develop resistencies. | ||
==Use== | ==Use== | ||