Kanthala Shanthi, Pallerla Sandeep, Jois Seetharama
Basic Pharmaceutical Sciences, School of Pharmacy, University of Louisiana at Monroe, Monroe, LA 71201, USA.
Future Oncol. 2015;11(5):865-78. doi: 10.2217/fon.14.312.
Expression of the EGF receptors (EGFRs) is abnormally high in many types of cancer, including 25% of lung cancers. Successful treatments target mutations in the EGFR tyrosine kinase domain with EGFR tyrosine kinase inhibitors (TKIs). However, almost all patients develop resistance to this treatment, and acquired resistance to first-generation TKI has prompted the clinical development of a second generation of EGFR TKI. Because of the development of resistance to treatment of TKIs, there is a need to collect genomic information about EGFR levels in non-small-cell lung cancer patients. Herein, we focus on current molecular targets that have therapies available as well as other targets for which therapies will be available in the near future.
表皮生长因子受体（EGFR）在包括25%的肺癌在内的多种癌症中表达异常高。成功的治疗方法是使用EGFR酪氨酸激酶抑制剂（TKIs）靶向EGFR酪氨酸激酶结构域中的突变。然而，几乎所有患者都会对这种治疗产生耐药性，对第一代TKI的获得性耐药促使了第二代EGFR TKI的临床研发。由于对TKIs治疗产生了耐药性，因此需要收集非小细胞肺癌患者中EGFR水平的基因组信息。在此，我们关注目前有可用疗法的分子靶点以及在不久的将来会有可用疗法的其他靶点。
