[3] CDK4/6抑制剂治疗激素受体阳性人表皮生长因子受体2阴性乳腺癌临床应用专家共识(2023版)[4] 中国临床肿瘤协会CSCO乳腺癌诊疗指南2023[5]Grinshpun,A.,Tolaney,S.M.,Burstein, H.J. et al. The dilemma of selecting a first line CDK4/6 inhibitor for hormone receptor-positive/HER2-negative ...
“新生”具有高水平 CDK2 活性的细胞可能不需要 CDK4/6 进行增殖,这一观察结果可能解释了 CDK4/6 抑制剂在源自此类细胞的肿瘤中缺乏活性的原因。 3. CDK4/6 在乳腺癌中的应用 在癌症中成功抑制 CDK4/6 信号依赖于完整的细胞周期蛋白 D-CDK4/6-RB1 轴,以及细胞类型对 CDK4/6 的特异性依赖性,以便通过...
CDK4/6 在控制细胞周期的 G1-S 周期转变中的主导作用高度依赖于细胞类型。单个Cdk4 或 Cdk6小鼠敲除是非致命的,反映了 CDK4 和 CDK6 之间的很大程度的功能补偿。然而,Cdk4 和Cdk6的双重敲除导致胚胎晚期严重、致命的贫血,尽管非血...
[9] Bidard FC, Hardy-Bessard AC, Dalenc F, et al. Switch to fulvestrant and palbociclib versus no switch in advanced breast cancer with rising ESR1 mutation during aromatase inhibitor and palbociclib therapy (PADA-1): a randomised, open-label, multicentre, phase 3 trial. Lancet Oncol. 2022...
20. Cai Z, Wang J, Li Y, et al. Overexpressed Cyclin D1 and CDK4 proteins are responsible for the resistance to CDK4/6 inhibitor in breast cancer that can be reversed by PI3K/mTOR inhibitors. Sci China Life Sci...
2.CDK4/6 inhibitor resistance mechanisms and treatment strategies. DOI: 10.3892/ijmm.2022.5184 5.CDK4/6 inhibitors in HER2-positive breast cancer. Critical Reviews in Oncology/Hematology 112 (2017) 208–214 DOI:10.1016/j.critrevonc.2017.02.022...
[2] Finn, R. PD0332991, a Selective Cyclin D Kinase 4/6 Inhibitor, Preferentially Inhibits Proliferation of Luminal Estrogen Receptor-Positive Human Breast Cancer Cell Lines in Vitro. Breast Cancer Research. 2009; R77.[3] 康建磊,王彦明.首个CDK4/6抑制剂新药——Palbociclib[J].临床药物治疗杂志,...
近日，来自美国辉瑞全球研发中心的Stephen G. Dann团队和Todd VanArsdale团队在Cancer Cell杂志上合作发表了一篇题为 Expanding control of the tumor cell cycle with a CDK2/4/6 inhibitor 的文章，这项研究通过临床前模型和临床转录组样本的分析揭示由MYC和CDK2的激活引发对CDK4/6抑制剂的耐药性。此外，该团队...
[1]Kevin Kalinsky, et al.Abemaciclib plus fulvestrant vs fulvestrant alone for HR+, HER2- advanced breast cancer following progression on a prior CDK4/6 inhibitor plus endocrine therapy: Primary outcome of the phase 3 postMONARCH trial.J Clin Oncol 42, 2024 (suppl 17; abstr LBA1001) ...
国内目前共有4款用于乳腺癌治疗的CDK4/6抑制剂上市：哌柏西利、阿贝西利、达尔西利、瑞波西利。这些药物的获批适应证分别是：哌柏西利：HR+/HER2-局部晚期或转移性乳腺癌，与芳香化酶抑制剂（aromataseinhibitor，AI）联用作为绝经后女性患者的初始内分泌治疗。阿贝西利：联合内分泌治疗用于HR+/HER2-部分早期乳腺癌...