Sun Guang-Chun, Yang Xu, Yu Yan, Zhao Dai-Wei
Department of Pharmacy, The Fifth People's Hospital of Shanghai, Fudan University; 801 He-Qing Rd., Shanghai 200240, China.
Anticancer Agents Med Chem. 2015;15(7):869-80. doi: 10.2174/1871520615666150318101845.
Anti-cancer targeting drugs appear to be a new and powerful "weapon" for cancer therapies. These targeting drugs are directed against specific molecules that are over-expressed or where certain unique factors are aberrantly expressed either in cancer cells or in diseased cell sites. Compared with traditional chemotherapeutic drugs, these targeting drugs have the advantages of high specificity, efficacy and less side effects. Target therapy is a breakthrough and revolutionary advance in the field of cancer therapy. Tumor angiogenesis plays a key role in tumor growth and metastasis and the mutation of tyrosine kinases is also strongly associated with cancer progression. Thus, in this review, we will discuss the advances in the development of targeting anti-cancer drugs by narrowing it down to small molecule tyrosine kinase inhibitors, monoclonal antibodies against epidermal growth factor receptors belonging to the ErbB family of receptor tyrosine kinases and angiogenic inhibitors. It will also address concerns for drug resistance and adverse events.
抗癌靶向药物似乎是癌症治疗中一种新型且强大的“武器”。这些靶向药物针对癌细胞或病变细胞部位中过度表达的特定分子,或某些独特因子异常表达的情况。与传统化疗药物相比,这些靶向药物具有高特异性、高效性和较少副作用的优点。靶向治疗是癌症治疗领域的一项突破性和革命性进展。肿瘤血管生成在肿瘤生长和转移中起关键作用,酪氨酸激酶的突变也与癌症进展密切相关。因此,在本综述中,我们将通过聚焦小分子酪氨酸激酶抑制剂、针对属于受体酪氨酸激酶ErbB家族的表皮生长因子受体的单克隆抗体和血管生成抑制剂,来讨论抗癌靶向药物的研发进展。它还将探讨耐药性和不良事件问题。