Overexpression of epidermal growth factor receptor (EGFR), a transmembrane
receptor tyrosine kinase, is prevalent in malignant tumors of epithelial
origin and is especially common in breast, head and neck, colon, and lung cancer.
With EGFR overexpression, prognosis is poor due to associated tumor invasion,
metastasis, enhanced angiogenesis, and resistance to chemotherapy; thus,
modulation of EGFR-mediated signaling is an attractive target for intervention.
Small-molecule kinase inhibitors (gefitinib and erlotinib) and a monoclonal
antibody (cetuximab) specific for EGFR are in clinical evaluation, but treatment
cessation due to development of severe acne-like rash is common with these
EGFR antagonists. Notably, nimotuzumab, a humanized form of the murine
IgG2a monoclonal antibody that has been launched in India for treatment of head
and neck cancers overexpressing EGFR, demonstrates clinical efficacy devoid of
the rash toxicity.
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