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Gefitinib response

MedGen UID:
450459
•Concept ID:
CN077987
•
Sign or Symptom
Synonym: Iressa response
Drug:
Gefitinib
MedGen UID:
209468
•Concept ID:
C1122962
•
Pharmacologic Substance
An anilinoquinazoline with antineoplastic activity. Gefitinib inhibits the catalytic activity of numerous tyrosine kinases including the epidermal growth factor receptor (EGFR), which may result in inhibition of tyrosine kinase-dependent tumor growth. Specifically, this agent competes with the binding of ATP to the tyrosine kinase domain of EGFR, thereby inhibiting receptor autophosphorylation and resulting in inhibition of signal transduction. Gefitinib may also induce cell cycle arrest and inhibit angiogenesis. (NCI04) [from NCI]
Gefitinib

Professional guidelines

PubMed

Autophagy as a molecular target for cancer treatment.
Kocaturk NM, Akkoc Y, Kig C, Bayraktar O, Gozuacik D, Kutlu O
Eur J Pharm Sci 2019 Jun 15;134:116-137. Epub 2019 Apr 11 doi: 10.1016/j.ejps.2019.04.011. PMID: 30981885
Role of osimertinib in the treatment of EGFR-mutation positive non-small-cell lung cancer.
Carlisle JW, Ramalingam SS
Future Oncol 2019 Mar;15(8):805-816. Epub 2019 Jan 18 doi: 10.2217/fon-2018-0626. PMID: 30657347
Management of acquired resistance to EGFR TKI-targeted therapy in advanced non-small cell lung cancer.
Wu SG, Shih JY
Mol Cancer 2018 Feb 19;17(1):38. doi: 10.1186/s12943-018-0777-1. PMID: 29455650Free PMC Article

Curated

DailyMed Drug Label, gefitinib, 2021

Recent clinical studies

Etiology

Silencing of miR490-3p by H. pylori activates DARPP-32 and induces resistance to gefitinib.
Zhu S, Khalafi S, Chen Z, Poveda J, Peng D, Lu H, Soutto M, Que J, Garcia-Buitrago M, Zaika A, El-Rifai W
Cancer Lett 2020 Oct 28;491:87-96. Epub 2020 Jul 29 doi: 10.1016/j.canlet.2020.07.014. PMID: 32735911Free PMC Article
Defining a Radiomic Response Phenotype: A Pilot Study using targeted therapy in NSCLC.
Aerts HJ, Grossmann P, Tan Y, Oxnard GR, Rizvi N, Schwartz LH, Zhao B
Sci Rep 2016 Sep 20;6:33860. doi: 10.1038/srep33860. PMID: 27645803Free PMC Article
The Dissociation of Gefitinib Trough Concentration and Clinical Outcome in NSCLC Patients with EGFR Sensitive Mutations.
Xin S, Zhao Y, Wang X, Huang Y, Zhang J, Guo Y, Li J, Li H, Ma Y, Chen L, Hu Z, Huang M, Zhang L
Sci Rep 2015 Jul 31;5:12675. doi: 10.1038/srep12675. PMID: 26228025Free PMC Article
Correlations of EGFR mutations and increases in EGFR and HER2 copy number to gefitinib response in a retrospective analysis of lung cancer patients.
Pugh TJ, Bebb G, Barclay L, Sutcliffe M, Fee J, Salski C, O'Connor R, Ho C, Murray N, Melosky B, English J, Vielkind J, Horsman D, Laskin JJ, Marra MA
BMC Cancer 2007 Jul 13;7:128. doi: 10.1186/1471-2407-7-128. PMID: 17626639Free PMC Article
Novel heteroduplex method using small cytology specimens with a remarkably high success rate for analysing EGFR gene mutations with a significant correlation to gefitinib efficacy in non-small-cell lung cancer.
Oshita F, Matsukuma S, Yoshihara M, Sakuma Y, Ohgane N, Kameda Y, Saito H, Yamada K, Tsuchiya E, Miyagi Y
Br J Cancer 2006 Oct 23;95(8):1070-5. doi: 10.1038/sj.bjc.6603396. PMID: 17047654Free PMC Article

Diagnosis

Leucine Zipper Downregulated in Cancer-1 Interacts with Clathrin Adaptors to Control Epidermal Growth Factor Receptor (EGFR) Internalization and Gefitinib Response in EGFR-Mutated Non-Small Cell Lung Cancer.
Huang HN, Hung PF, Chen YP, Lee CH
Int J Mol Sci 2024 Jan 23;25(3) doi: 10.3390/ijms25031374. PMID: 38338651Free PMC Article
Clathrin-mediated EGFR endocytosis as a potential therapeutic strategy for overcoming primary resistance of EGFR TKI in wild-type EGFR non-small cell lung cancer.
Kim B, Park YS, Sung JS, Lee JW, Lee SB, Kim YH
Cancer Med 2021 Jan;10(1):372-385. Epub 2020 Dec 12 doi: 10.1002/cam4.3635. PMID: 33314735Free PMC Article
EGFR endocytosis is a novel therapeutic target in lung cancer with wild-type EGFR.
Jo U, Park KH, Whang YM, Sung JS, Won NH, Park JK, Kim YH
Oncotarget 2014 Mar 15;5(5):1265-78. doi: 10.18632/oncotarget.1711. PMID: 24658031Free PMC Article
Predicting differences in gene regulatory systems by state space models.
Yamaguchi R, Imoto S, Yamauchi M, Nagasaki M, Yoshida R, Shimamura T, Hatanaka Y, Ueno K, Higuchi T, Gotoh N, Miyano S
Genome Inform 2008;21:101-13. PMID: 19425151
Novel heteroduplex method using small cytology specimens with a remarkably high success rate for analysing EGFR gene mutations with a significant correlation to gefitinib efficacy in non-small-cell lung cancer.
Oshita F, Matsukuma S, Yoshihara M, Sakuma Y, Ohgane N, Kameda Y, Saito H, Yamada K, Tsuchiya E, Miyagi Y
Br J Cancer 2006 Oct 23;95(8):1070-5. doi: 10.1038/sj.bjc.6603396. PMID: 17047654Free PMC Article

Therapy

Leucine Zipper Downregulated in Cancer-1 Interacts with Clathrin Adaptors to Control Epidermal Growth Factor Receptor (EGFR) Internalization and Gefitinib Response in EGFR-Mutated Non-Small Cell Lung Cancer.
Huang HN, Hung PF, Chen YP, Lee CH
Int J Mol Sci 2024 Jan 23;25(3) doi: 10.3390/ijms25031374. PMID: 38338651Free PMC Article
Systemic therapy for advanced cutaneous squamous cell carcinoma.
Fitzgerald K, Tsai KK
Semin Cutan Med Surg 2019 Mar 1;38(1):E67-E74. doi: 10.12788/j.sder.2019.010. PMID: 31051028
EGFR endocytosis is a novel therapeutic target in lung cancer with wild-type EGFR.
Jo U, Park KH, Whang YM, Sung JS, Won NH, Park JK, Kim YH
Oncotarget 2014 Mar 15;5(5):1265-78. doi: 10.18632/oncotarget.1711. PMID: 24658031Free PMC Article
Predicting differences in gene regulatory systems by state space models.
Yamaguchi R, Imoto S, Yamauchi M, Nagasaki M, Yoshida R, Shimamura T, Hatanaka Y, Ueno K, Higuchi T, Gotoh N, Miyano S
Genome Inform 2008;21:101-13. PMID: 19425151
Novel heteroduplex method using small cytology specimens with a remarkably high success rate for analysing EGFR gene mutations with a significant correlation to gefitinib efficacy in non-small-cell lung cancer.
Oshita F, Matsukuma S, Yoshihara M, Sakuma Y, Ohgane N, Kameda Y, Saito H, Yamada K, Tsuchiya E, Miyagi Y
Br J Cancer 2006 Oct 23;95(8):1070-5. doi: 10.1038/sj.bjc.6603396. PMID: 17047654Free PMC Article

Prognosis

Leucine Zipper Downregulated in Cancer-1 Interacts with Clathrin Adaptors to Control Epidermal Growth Factor Receptor (EGFR) Internalization and Gefitinib Response in EGFR-Mutated Non-Small Cell Lung Cancer.
Huang HN, Hung PF, Chen YP, Lee CH
Int J Mol Sci 2024 Jan 23;25(3) doi: 10.3390/ijms25031374. PMID: 38338651Free PMC Article
EGFR endocytosis is a novel therapeutic target in lung cancer with wild-type EGFR.
Jo U, Park KH, Whang YM, Sung JS, Won NH, Park JK, Kim YH
Oncotarget 2014 Mar 15;5(5):1265-78. doi: 10.18632/oncotarget.1711. PMID: 24658031Free PMC Article
Characterization and response of newly developed high-grade glioma cultures to the tyrosine kinase inhibitors, erlotinib, gefitinib and imatinib.
Kinsella P, Howley R, Doolan P, Clarke C, Madden SF, Clynes M, Farrell M, Amberger-Murphy V
Exp Cell Res 2012 Mar 10;318(5):641-52. Epub 2012 Jan 20 doi: 10.1016/j.yexcr.2012.01.014. PMID: 22285130
Predicting differences in gene regulatory systems by state space models.
Yamaguchi R, Imoto S, Yamauchi M, Nagasaki M, Yoshida R, Shimamura T, Hatanaka Y, Ueno K, Higuchi T, Gotoh N, Miyano S
Genome Inform 2008;21:101-13. PMID: 19425151
Novel heteroduplex method using small cytology specimens with a remarkably high success rate for analysing EGFR gene mutations with a significant correlation to gefitinib efficacy in non-small-cell lung cancer.
Oshita F, Matsukuma S, Yoshihara M, Sakuma Y, Ohgane N, Kameda Y, Saito H, Yamada K, Tsuchiya E, Miyagi Y
Br J Cancer 2006 Oct 23;95(8):1070-5. doi: 10.1038/sj.bjc.6603396. PMID: 17047654Free PMC Article

Clinical prediction guides

Defining a Radiomic Response Phenotype: A Pilot Study using targeted therapy in NSCLC.
Aerts HJ, Grossmann P, Tan Y, Oxnard GR, Rizvi N, Schwartz LH, Zhao B
Sci Rep 2016 Sep 20;6:33860. doi: 10.1038/srep33860. PMID: 27645803Free PMC Article
EGFR endocytosis is a novel therapeutic target in lung cancer with wild-type EGFR.
Jo U, Park KH, Whang YM, Sung JS, Won NH, Park JK, Kim YH
Oncotarget 2014 Mar 15;5(5):1265-78. doi: 10.18632/oncotarget.1711. PMID: 24658031Free PMC Article
Quantitative proteomic profiling identifies protein correlates to EGFR kinase inhibition.
Kani K, Faca VM, Hughes LD, Zhang W, Fang Q, Shahbaba B, Luethy R, Erde J, Schmidt J, Pitteri SJ, Zhang Q, Katz JE, Gross ME, Plevritis SK, McIntosh MW, Jain A, Hanash S, Agus DB, Mallick P
Mol Cancer Ther 2012 May;11(5):1071-81. Epub 2012 Mar 12 doi: 10.1158/1535-7163.MCT-11-0852. PMID: 22411897Free PMC Article
Predicting differences in gene regulatory systems by state space models.
Yamaguchi R, Imoto S, Yamauchi M, Nagasaki M, Yoshida R, Shimamura T, Hatanaka Y, Ueno K, Higuchi T, Gotoh N, Miyano S
Genome Inform 2008;21:101-13. PMID: 19425151
Correlations of EGFR mutations and increases in EGFR and HER2 copy number to gefitinib response in a retrospective analysis of lung cancer patients.
Pugh TJ, Bebb G, Barclay L, Sutcliffe M, Fee J, Salski C, O'Connor R, Ho C, Murray N, Melosky B, English J, Vielkind J, Horsman D, Laskin JJ, Marra MA
BMC Cancer 2007 Jul 13;7:128. doi: 10.1186/1471-2407-7-128. PMID: 17626639Free PMC Article

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