Melanoma Molecular Maps Projects



Title: List of EGFR inhibitors
Legend: The HER (human epidermal growth factor receptor) family of membrane tyrosine kinase receptors (TKR) includes the epidermal growth factor receptor (EGFR, also called HER1, ErbB1), HER2 (ErbB2, HER2, neu), HER3 (ErbB3), and HER4 (ErbB4). Epidermal growth factor (EGF), transforming growth factor (TGF) alpha, and amphiregulin bind exclusively to the EGFR, whereas betacellulin and epiregulin bind both the EGFR and HER4. HER2 does not bind to any known ligand, but it is the preferred heterodimerization partner for EGFR after ligand-induced activation. The intracellular signaling transduced by EGFR activation stimulates cell proliferation, promotes angiogenesis, and opposes apoptosis, which ultimately favor tumor growth and metastasis development. The EGFR pathway is dysregulated in many malignancies including melanoma, although the expression of the two most studied HER family members by melanoma cells is generally reported to be moderate (EGFR) to low (HER2). Several anti-EGFR agents are being developed, such as AEE788, canertinib (CI-1033), cetuximab (IMC-C225, Erbitux (R)), EKB-569, erlotinib (OSI-774, Tarceva (R)), gefitinib (ZD1839, Iressa (R)), lapatinib (GW572016, Tykerb (R)), mAb806, matuzumab (EMD-72000), MDX-477, nimotuzumab (h-R3), panitumumab (ABX-EGF, Vectibix (R)), PD153035, PKI-166). Some of them are approved for the routine clinical treatment of some carcinomas. TKI: tyrosine kinase inhibitor; VEGFR: vascular endothelial growth factor receptor. REFERENCES: [1] Hynes NE et al, Nat Rev Cancer 2005, 5:341-54. [2] Rocha-Lima C et al, Cancer Control 2007, 14:295-304. [3] Harari PM et al, J Clin Oncol 2007, 25:4057-65
Author: MMMP Team (updated: Nov 2007)

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