以EGFR为靶点的肿瘤分子靶向药物研究进展

随着分子生物学研究的进展,分子靶向治疗已成为除手术、放疗、化疗之外的第4种治疗方法,越来越多的用于临床治疗恶性肿瘤。分子靶向药物进入体内能够特异地选择致癌位点,杀伤肿瘤细胞,而不会波及周围正常的组织细胞,因此分子靶向治疗又被称为"生物导弹"。与传统化疗药物相比,分子靶向药物具有特异性强、疗效明显、副作用少等优点。按照分子靶向药物的性质主要归为两大类:一类是单克隆抗体,如西妥昔单抗等;另一类是单靶点或多靶点的小分子抑制剂,如吉非替尼等。表皮生长因子受体(EGFR)对肿瘤的生长、发展以及肿瘤干细胞的维持都有着非常重要的作用,并且在多种实体瘤中存在过表达或异常表达,因此在肿瘤治疗中,EGFR成为一个非常重要的用药靶点。现主要对目前国内已上市的针对EGFR的分子靶向药物最新的临床研究进展作一简要综述。

Recent Development of Molecular Targeted Cancer Drugs Targeted EGFR

With the progress of molecular biology,there is a growing number of molecular targeted cancer drugs have been used in clinical to treat of malignant tumors.Molecular targeted therapy is also known as "biological missile",and has become the fourth treatment methods in addition to surgery,radiotherapy and chemotherapy.Compared with traditional chemotherapy drugs,the advantages of molecular targeted drugs are specificity,efficacy and less side effects.Molecular targeted drugs can be divided into two classes according to the nature: monoclonal antibodies such as cetuximab and small molecule inhibitors with single target or multiple targets such as gefitinib.The epidermal growth factor receptor(EGFR) has been found that it contributes to tumor cell survival,proliferation,and motility.Overexpression and mutation of the EGFR gene are the most common mechanisms by which EGFR exerts influence on tumorigenesis.Therefore,EGFR has been successfully targeted for cancer therapy.The latest clinical research of the molecular targeted drugs have been listed targeted epidermal growth factor receptor(EGFR).