INHIBITORS OF THE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) WITH CYTOSTATIC ACTION AND THEIR USES IN TUMOUR THERAPY.

摘要

The present invention relates to inhibitors of the Epidermal Growth Factor Receptor (EGFR) which bond to the receptor by domains I or III blocking the bonding of the natural ligands but which permit physiological equilibrium between the inactive and active conformations of the receptor such as to prevent the mitogenic signal but the fraction of domain II of the receptors in active conformation homodimerise and autophosphorylate the receptor triggering the chain of biochemical events which maintain cell survival. The authors of this invention have found that these inhibitors which recognise the EGFR by domains I or III have a cytostatic and not a cytotoxic effect on tumours which express said receptor and represent an advantage over the state of the art because the adverse effects which they bring about are less significant than those reported.