A novel approach in the treatment of cancer: targeting the epidermal growth factor receptor.

By Fortunato Ciardiello, G. Tortora. Clinical Cancer Research, 2001

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ZD6474, an orally available inhibitor of KDR tyrosine kinase activity, efficiently blocks oncogenic RET kinases. (2002, background): “Phase I and II trials in patients with advanced disease have demonstrated that an anilinoquinazoline-derivative, ZD1839, has a good tolerability profile and a promising clinical efficacy in patients with diverse types of tumors (14).”
ZD1839 (Iressa): an orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy. (2002, background): “In the 15 years since EGFR(3) (erbB1) was recognized as the cellular homologue of the viral oncogene v-erb, two strands of research have come together to make a compelling case for EGFR as an attractive target for cancer chemotherapy (1, 2).”
Phase II trial of gefitinib in recurrent glioblastoma. (2004, background): “Gefitinib (ZD1839, Iressa; AstraZeneca, Wilmington, DE) is a novel, oral low–molecular weight, adenosine triphosphate mimetic of the anilinoquinazoline family that reversibly inhibits the tyrosine kinase activity associated with EGFR [7,8].”
Mechanisms of receptor tyrosine kinase activation in cancer (2018, unknown): “Autocrine pathways could act as a rational target for cancer therapy [151].”
Mutations of the Epidermal Growth Factor Receptor Gene in Lung Cancer (2004, background): “Gefitinib is an orally administered small molecule that specifically inhibits EGFR tyrosine phosphorylation (3).”