Institute of Medical Science and Technology, National Sun Yat-sen University, Kaohsiung 80424, Taiwan.
Institute of Biomedical Sciences, Academia Sinica, Taipei 11529, Taiwan.
J Control Release. 2020 Aug 10;324:482-492. doi: 10.1016/j.jconrel.2020.05.043. Epub 2020 Jun 1.
Lung cancer is the primary cause of cancer-related death worldwide. 85%-90% of cases are non-small cell lung cancer (NSCLC) which characteristically exhibits altered epidermal growth factor receptor (EGFR) signaling is a major driver pathway. Unfortunately, therapeutic outcomes in treating NSCLC are compromised by the emergence of drug resistance in response to EGFR-tyrosine kinase inhibitor (TKI) targeted therapy due to the acquired resistance mutation EGFR T790M or activation of alternative pathways. There is current need for a new generation of TKIs to be developed to treat EGFR-TKI-resistant NSCLC. To overcome the above problems and improve clinical efficacy, nanotechnology with targeting abilities and sustained release has been proposed for EGFR-TKI-resistant NSCLC treatment and has already achieved success in in vitro or in vivo models. In this review, we summarize and illustrate representative nano-formulations targeting EGFR-TKI-resistant NSCLC. The described advances may pave the way to better understanding and design of nanocarriers and multifunctional nanosystems for efficient treatment for drug resistant NSCLC.
肺癌是全球癌症相关死亡的主要原因。85%-90%的病例是非小细胞肺癌(NSCLC),其特征是表皮生长因子受体(EGFR)信号改变,是主要的驱动途径。不幸的是,由于获得性耐药突变 EGFR T790M 或其他途径的激活,针对 EGFR-酪氨酸激酶抑制剂(TKI)的靶向治疗药物的出现,导致对 NSCLC 的治疗出现耐药,从而影响了治疗效果。目前需要开发新一代 TKI 来治疗 EGFR-TKI 耐药的 NSCLC。为了克服上述问题并提高临床疗效,具有靶向能力和持续释放的纳米技术已被提议用于治疗 EGFR-TKI 耐药的 NSCLC,并已在体外或体内模型中取得成功。在这篇综述中,我们总结并说明了针对 EGFR-TKI 耐药 NSCLC 的代表性纳米制剂。所描述的进展可能为更好地理解和设计用于有效治疗耐药 NSCLC 的纳米载体和多功能纳米系统铺平道路。