TargetingKRASG12Dmutation in non-small cell lung cancer: molecular mechanisms and therapeutic potentialLung malignant tumors are a type of cancer with high incidence and mortality rates worldwide. Non-small cell lung cancer (NSCLC) accounts for over 80% of all lung malignant tumors, and most ...
与非KRAS G12D突变相比,KRAS G12D突变的NSCLC患者更常见EGFR(25% vs 8.8%;P=0.124)和CDKN2A(18.8% vs 5.9%;P=0.157)基因的突变,而TP53丢失(58.8% vs 37.5%;P=0.157)和STK11(23.5% vs 6.3%;P=0.138)突变更容易发生在非KRAS G12D突变患者中。且携KRAS G12D突变的患者相较非KRAS G12D突变的患者具有...
这就要求,一方面需要创新,开发新型的、高效、广谱的KRAS抑制剂,(而不仅仅作为一个搅局者,为了卷而卷);另一方面需要研究KRASG12D不同抑制剂的作用机制,以及联合用药的可能,和开发,更好的服务于疾病的治疗。 参考文献: 1)A Small Molecule with Big Impact: MRTX1133 ...
参考文献:Wang R, Cong D, Bai Y and Zhang W (2023) Case report: long-term sustained remission in a case of metastatic colon cancer with high microsatellite instability and KRAS exon 2 p.G12D mutation treated with fruquintinib after local radiotherapy: a case report and literature review. ...
参考文献:Wang R, Cong D, Bai Y and Zhang W (2023) Case report: long-term sustained remission in a case of metastatic colon cancer with high microsatellite instability and KRAS exon 2 p.G12D mutation treated with fruquintinib after local radiotherapy: a case report and literature review. ...
目前，针对KRAS G12C靶点的研究方兴未艾，而对KRAS G12D等其他靶点的探索以及泛RAS抑制剂的研发也已进入临床开发阶段。MRTX1133是Mirati Therapeutics研发的一款选择性非共价 KRAS G12D 抑制剂，目前已经获得了FDA 批准，获得新药临床试验申请批准，在 2023 年已经开始进入 I/II 期临床阶段。临床前研究结果显示：...
there are several mutations. The KRAS-G12C mutation, in particular, predominates in NSCLC (45–50% of mutant KRAS-G12C). On the other hand, KRAS-G12D (where glycine at codon-12 has mutated to aspartate), is important in pancreatic cancer (61%), colon cancer (42%), and NSCLC (22...
4月19日,劲方医药宣布该公司自主研发的KRAS G12C抑制剂GFH925单药疗法获得美国FDA临床试验许可,可针对KRAS G12C突变型难治、转移性结直肠癌患者开展一项多中心、开放标签、随机对照3期试验。此项试验将入组既往经两线或以上系统性治疗失败、或对末...
there are several mutations. The KRAS-G12C mutation, in particular, predominates in NSCLC (45–50% of mutant KRAS-G12C). On the other hand, KRAS-G12D (where glycine at codon-12 has mutated to aspartate), is important in pancreatic cancer (61%), colon cancer (42%), and NSCLC (22...
表3:正在开展的KRASG12C抑制剂联合其它药物的临床研究 参考文献 1. Muzny DM, et al. Comprehensive molecular characterization of human colon and rectal cancer. Nature. 2012 Jul 18;487(7407):330-7. 2. Cervantes A, e...