Boland William Kells, Bebb Gwyn
McGill University, Anatomy and Cell Biology, Montreal, Quebec, Canada.
Expert Opin Biol Ther. 2009 Sep;9(9):1199-206. doi: 10.1517/14712590903110709.
Due to the broad importance of EGFR to tumorogenesis, targeted therapy against it has rapidly developed into a novel paradigm for cancer treatment. Two promising classes of drugs are now in use and undergoing development that target this receptor: tyrosine kinase inhibitors (TKIs) and mAbs that inhibit EGFR's extracellular domain. Nimotuzumab, a humanized murine mAb created in Cuba, has demonstrated antitumor activity similar to that of other anti-EGFR mAbs and shows promise as a single agent and as an adjunct to radiation in Phase I and II clinical trials. Surprisingly, the typical severe dermatological toxicities thus far associated with anti-EGFR therapy have not been described with nimotuzumab. Here we summarize the background, development and characteristics of this new drug while reviewing the latest preclinical and clinical trial data that underpin its gradual adoption into clinical practice.
由于表皮生长因子受体(EGFR)在肿瘤发生过程中具有广泛的重要性,针对它的靶向治疗已迅速发展成为一种新型癌症治疗模式。目前有两类很有前景的药物正在使用并处于研发阶段,它们靶向这种受体:酪氨酸激酶抑制剂(TKIs)和抑制EGFR胞外结构域的单克隆抗体(mAbs)。尼妥珠单抗是一种在古巴研制的人源化鼠单克隆抗体,已显示出与其他抗EGFR单克隆抗体相似的抗肿瘤活性,并且在I期和II期临床试验中作为单一药物以及放疗辅助药物都展现出前景。令人惊讶的是,迄今为止,尼妥珠单抗尚未出现与抗EGFR治疗相关的典型严重皮肤毒性。在此,我们总结这种新药的背景、研发和特性,同时回顾最新的临床前和临床试验数据,这些数据支撑着它逐渐被应用于临床实践。