作为一个关键的克隆致癌驱动因子,KRAS基因是中国NSCLC人群中第二常见的突变基因,其突变主要发生在第12、13和61位氨基酸残基位点,在所有的KRAS突变亚型中,G12C是其主要的突变亚型²。自KRAS靶点发现以来,长达40年均无靶向药物获批,但近几年多款KRAS G12C抑制剂的问世,打破了KRAS靶点“不可成药”的魔咒,为KRAS G...
The KRAS glycine-to-cysteine mutation (KRAS G12C) comprises approximately 44% of KRAS mutations in NSCLC, with mutant KRASG12C present in approximately 13% of all patients with lung adenocarcinoma. Mutant KRAS has been an oncogenic target for decades, but no viable therapeutic agents were ...
~ 13% (1 in 8) of patients with non-squamous NSCLC have the KRAS G12C mutation, yet too many of these patients go unidentified. Consider testing for all actionable mutations in eligible patients with NSCLC at diagnosis and help Find KRAS G12C....
n = number of NSCLC samples positive for KRAS G12C mutation. N1 = number of NSCLC samples with any KRAS mutation. *Only patients with a KRAS mutation were recruited. †Included patients who had no other known druggable mutations. FH-FMI CGDB, Flatiron Health-Foundation Medicine ...
Sotorasib最近获得了美国食品和药物管理局(FDA)的加速批准,用于治疗患有KRAS G12C突变、局部晚期或转移性NSCLC的成年患者。2此外,首个针对G12D突变的药物正在开发中。然而,就目前而言,大多数KRAS突变晚期NSCLC患者的治疗选择仍仅限于化疗和免疫疗法。 KRAS突变NSCLC的治疗方案...
不管是G12C还是G12D项目,本质上都是聚焦于KRAS突变亚型精准靶向,而Pan-(K)RAS抑制剂则代表了另一种开发思路,可以覆盖更多突变类型,也有希望更深入地克服耐药问题。 理论上,Pan-(K)RAS抑制剂覆盖的潜在患者群体更大,自然而然背后的市场空间也更大。而且,似乎各类选择性KRAS抑制剂瞄准的适应人群,也在这些泛抑制...
在主席论坛专场上,斯隆凯特琳癌症中心Bob T. L教授公布了II期CodeBreak 100试验的结果:在KRAS G12C突变的晚期非小细胞肺癌患者中,使用KRAS G12C抑制剂Sotorasib(AMG 510)治疗可获得6.8个月的中位无进展生存期(PFS)。 今天,我们有...
Expert perspectives on the management of KRAS G12C–mutant non–small cell lung cancer in the context of novel targeted agents. EP: 1.Optimal Molecular Testing Practices in Non–Small Cell Lung Cancer EP: 2.Real-World Data and Barriers to Use of Molecular Testing in NSCLC EP: 3.Use of ...
Interestingly, the KRAS G12C mutation was clonal, whereas the KRAS G12V was observed at subclonal level, indicating KRAS codon 12 can be hit twice in the same cell during the course of NSCLC development23. The KRAS protein change then depends on which allele is hit the second time. ...
2019年ASCO, WCLC, ESMO中,安进先后更新KRAS G12C抑制剂AMG 510临床数据,打破了KRAS不可成药的魔咒,安进、辉瑞、BI等先后入局,KRAS G12C, KRAS G12D抑制剂一时成为炙手可热的研发项目。 KRAS是一个超百亿美元的全新市场,流行病学显示[1-3]1...