The present invention is related to inhibitors of the epidermal growth factor receptor (EGFR) that bind to either domain I or III of the receptor, blocking the binding of the natural ligands, but permitting the physiological equilibrium between the active and inactive receptor conformations, so that they inhibit the mitogenic signal, but the fraction of the receptors that adopt the active conformation still can dimerize and become phosphorylated, triggering the cascade of biochemical events that guarantee cell survival. The authors of this invention have found that these inhibitors that recognize the EGFR either by domain I or III have a cytostatic effect, rather than cytotoxic on tumors that express said receptor, and represent an advantage over the state of the art because the adverse effects they provoke are minor as compared to those previously reported.本發明關於表皮生長因子受體(EGFR)之抑制劑類,彼等與該受體之結構域I或III結合,藉以阻斷天然配位體之結合但仍允許該活化受體構型與不活化受體構型之間的生理平衡,因此該等抑制劑抑制細胞分裂信號,但是採取活化構型之受體部分仍可二聚化且變成磷酸化,藉以觸發確保細胞存活之生化事件的級聯。本發明之作者發現能辨識EGFR之結構域I或III之該等抑制劑類對表現該受體之腫瘤具有細胞生長抑制功效,而非細胞毒性作用,且該等抑制劑類代表超越現有技藝之優點,因為相較於先前所報告者,彼等抑制劑類所引起的不良反應極小。
