免疫治疗组合:第二代KRAS G12C抑制剂olomorasib与ICI 帕博利珠单抗联合使用显示出63%的ORR。提示该组合疗法可能具有良好的疗效。 化疗组合:sotorasib与铂类及培美曲塞联合治疗的ORR为65%,中位PFS为10.8个月。 其他靶向治疗组合:KRAS G12C抑制剂fulzerasib与EGFR抑制剂cetuximab的组合显示出80%的ORR,100%的DCR。
He Q, Liu X, et al. First-line treatments for KRAS-mutant non-small cell lung cancer: current state and future perspectives. Cancer Biol Ther. 2025 Dec;26(1):2441499. doi: 10.1080/15384047.2024.2441499. Epub 2024 Dec 16. 审校:Sq...
Among KRAS family proteins and mutants, both ITC and enzymatic assays demonstrate the selectivity of the inhibitors for KRAS(G12D); and the inhibitors disrupt the KRAS–CRAF interaction. We also observed the inhibition of cancer cell proliferation as well as MAPK signaling by a representative ...
Using mouse cell lines derived from Kras G12D and Kras G12D / Lkb1 / mouse models and the human lung cancer (A549) cell line, we show that ETS1 regulates Twist1 expression. Chromatin immunoprecipitation assays confirm binding of ETS1 to the Twist1 promoter. Overexpression studies show that...
这是一项Ⅰ期、剂量递增的首次人体研究,纳入了患有不可切除或转移性KRAS G12D阳性实体瘤的成人患者。患者接受ASP3082单药(10~600 mg)静脉给药,每周一次,每21天为一个周期。主要终点是剂量限制性毒性(DLT)和不良事件(AE)的发生率。 ...
针对KRAS G12C“圣杯”靶点,氟泽雷塞优势显著 KRAS突变包括诸多的位点突变,唐可京教授强调,第12号密码子位置的突变占KRAS突变的80%,包括G12A、G12C、G12D、G12V等突变亚型,其中,又以KRAS G12C为常见[6]。在KRAS突变NSCLC患者中,KRAS G12C突变的发生率达到了近40.0%[7]。2013年,Ostrem等人[8]在KRAS G12...
USAofsotorasibinMay2021.Sotorasib,aKRASG12C inhibitor,isindicatedforthetreatmentofadultswith KRASG12C-mutatedlocallyadvancedormetastatic non-smallcelllungcancer(NSCLC)whohavereceived atleastonepriorsystemictherapy.Theapprovalwas basedondatafromtheCodeBreaK100Phase1/2trial ...
KRAS在多种实体肿瘤中均会发生基因突变,其中胰腺导管腺癌发生突变的几率最高,突变形式包括KRAS-G12D、KRAS-G12C和KRAS-G12V等。而在非小细胞肺癌中,KRAS基因以KRAS-G12C点突变最为常见。当KRAS基因出现G12C点突变后,其本身具备的GTP水解酶活性就会丢失,进而激活RAF-MEK-ERK、PI3K-AKT-mTOR和Ral-GDS等多条...
评估GFH375在携带KRAS G12D 突变的晚期实体瘤患者中的安全性/耐受性、PK 和初步有效性,并确定GFH375 的 MTD 和/或 RP2D。 评估GFH375 在携带KRAS G12D 突变的晚期实体瘤患者中的有效性。 开始日期2024-07-02 申办/合作机构 劲方医药科技(上海)股份有限公司初创企业 ...
1. Burns Timothy F, Borghaei Hossein, Ramalingam Suresh S, et al. Targeting KRAS-Mutant Non-Small-Cell Lung Cancer: One Mutation at a Time, With a Focus on KRAS G12C Mutations.[J] .J Clin Oncol, 2020, 38: 4208-4218. 2. Der C J, Krontiris T G, Cooper G M, Transforming gen...