. Author manuscript; available in PMC: 2018 Sep 1.

Published in final edited form as: Cancer Metastasis Rev. 2017 Sep;36(3):463–473. doi: 10.1007/s10555-017-9687-8

Table II.

EGFR-targeted Tyrosine Kinase Inhibitors

Compound	Company	Description	Approval and Clinical Indications
Gefitinib Iressa (ZD1839)	AstraZeneca Pharmaceuticals	Reversible binding EGFR specific Oral medicine	2003: advanced or metastatic NSCLC
Erlotinib Tarceva (OSI-774)	Genentech Astellas	Reversible binding EGFR specific	2004: locally advanced or metastatic NSCLC; approved in combination with gemcitabine for locally advanced or metastatic pancreatic cancer
Lapatinib Tykerb	GlaxoSmithKline	Reversible binding Inhibition of HER2/neu and EGFR	2007- in combination for breast cancer patient on capecitabine
Lapatinib Tykerb	GlaxoSmithKline	Reversible binding Inhibition of HER2/neu and EGFR	2010- in combination with an aromatase inhibitor for HER2 and hormone receptor positive metastatic breast cancer
Afatinib	Boehringer Ingelheim Pharmaceuticals	Irreversible Pan-ErbB binding	2013: first-line treatment of metastatic NSCLC with EGFR exon 19 deletions or exon 21 (L858R) substitutions
Dasatinib (Sprycel)	Bristol-Myers Squibb	c-Scr kinases; thought to interfere with nuclear localization and of EGFR (Raju 2012)	2006: adult chromosome-positive chronic myelogenous leukemia (CP-CML) for which imatinib was ineffective
Dasatinib (Sprycel)	Bristol-Myers Squibb		2010: newly diagnosed CP-CML
Dacomitinib	Pfizer	Irreversible Pan-ErbB binding	Phase I, II and III trials for cancers including HNSCC, NSCLC, and glioblastoma multiforme
ASP8273	Astellas Pharma	Irreversible binding Affinity higher for EGFR activating and T790M mutations compared to wild type	Phase I, II, and III trials in NSCLC and solid malignancies