靶向 KRAS：抑制 KRAS 用于治疗非小细胞肺癌的合理策略
On target: Rational approaches to KRAS inhibition for treatment of non-small cell lung carcinoma.
机构信息
Division of Cancer Sciences, University of Manchester, Manchester, UK; Department of Medical Oncology, The Christie NHS Foundation Trust, Manchester, UK; Cancer Research UK Lung Cancer Centre of Excellence, Manchester and London, UK.
Department of Medicine, University of Chicago, Chicago, USA.
出版信息
Lung Cancer. 2021 Oct;160:152-165. doi: 10.1016/j.lungcan.2021.07.005. Epub 2021 Jul 16.
Non-small cell lung carcinoma (NSCLC) is a leading cause of cancer death. Approximately one-third of patients with NSCLC have a KRAS mutation. KRAS, the most common mutation, is found in ~13% of patients. While KRAS was long considered 'undruggable', several novel direct KRAS inhibitors have shown encouraging signs of efficacy in phase I/II trials and one of these (sotorasib) has recently been approved by the US Food and Drug Administration. This review examines the role of KRAS mutations in NSCLC and the challenges in targeting KRAS. Based on specific KRAS biology, it reports exciting progress, exploring the use of novel direct KRAS inhibitors as monotherapy or in combination with other targeted therapies, chemotherapy, and immunotherapy.
非小细胞肺癌（NSCLC）是癌症死亡的主要原因。大约三分之一的 NSCLC 患者存在 KRAS 突变。KRAS 是最常见的突变，约见于 13%的患者。虽然 KRAS 长期以来被认为是“不可成药”的，但几种新型的直接 KRAS 抑制剂在 I/II 期临床试验中显示出令人鼓舞的疗效迹象，其中一种（sotorasib）最近已被美国食品和药物管理局批准。这篇综述探讨了 KRAS 突变在 NSCLC 中的作用以及针对 KRAS 的挑战。基于特定的 KRAS 生物学，它报告了令人兴奋的进展，探索了新型直接 KRAS 抑制剂作为单一疗法或与其他靶向治疗、化疗和免疫疗法联合使用的可能性。
Zotero 插件