[8] Dickler MN, Tolaney SM, Rugo HS, et al. MONARCH 1, A Phase II Study of Abemaciclib, a CDK4 and CDK6 Inhibitor, as a Single Agent, in Patients with Refractory HR+/HER2- Metastatic Breast Cancer [published ...
abemaciclib 的中枢神经系统渗透浓度足以使 CDK4/6 的临床相关抑制已在临床研究中得到证实。这些药物之间的其他临床相关差异包括生物利用度和代谢的变化,因此由于消除半衰期较短(abemaciclib为18.3 h,palbociclib为29 h,ribociclib为32 h),因...
[4]. Schaer DA, Beckmann RP, Dempsey JA, Huber L, Forest A, Amaladas N, et al. The CDK4/6 Inhibitor Abemaciclib Induces a T Cell Inflamed Tumor Microenvironment and Enhances the Efficacy of PD-L1 Checkpoint Blockade. Cell Rep. 2018;22(11):2978-94.[5]. Goel S, DeCristo MJ, Watt...
英文名称Abemaciclib 储存温度避光,-20°C储存 运输条件超低温冰袋运输 作用类型抑制剂 作用机制细胞周期蛋白依赖性激酶 6 抑制剂 产品介绍 Abemaciclib highly selective inhibits the complexes CDK4/ cyclin D1 (IC50 =2 nmol/L) and CDK6/cyclin D1 (IC50 =10 nmol/L), with no activity against other CDK...
唯一获得 FDA 批准用作单一药物的 CDK4/6 抑制剂是 abemaciclib。该药物可作为晚期 HR+HER2− 乳腺癌患者的单药治疗,在内分泌治疗和化疗后发生进展后使用,尽管在美国以外仍未获得批准。该批准是基于MONARCH-1试验的数据。 3. 瑞博西利(ribociclib) III期MONALEESA-2试验旨在研究 ribociclib 加来曲唑(letrozole...
“Poster Spotlight 2: Personalizing CDK 4/6 Inhibitor Therapy for Patients with Metastatic Breast Cancer: Survival, QOL and Biomarkers”环节进行了壁报展示和讨论,本研究基于美国Flatiron Health电子健康记录衍生的Panoramic数据库,对HR+/HER2- MBC患者一线使用三种CDK4/6抑制剂(CDK4/6i;哌柏西利、瑞波西利、...
[16]Parrish KE, Pokorny J, Mittapalli RK, Bakken K, Sarkaria JN, Elmquist WF. Efflux transporters at the blood-brain barrier limit delivery and efficacy of cyclin-dependent kinase 4/6 inhibitor palbociclib (PD-0332991) in an orthotopic brain tumor model. J Pharmacol Exp Ther. 2015 Nov;355...
[8] Dickler MN, Tolaney SM, Rugo HS, et al. MONARCH 1, A Phase II Study of Abemaciclib, a CDK4 and CDK6 Inhibitor, as a Single Agent, in Patients with Refractory HR+/HER2- Metastatic Breast Cancer [published correction appears in Clin Cancer Res. 2018 Nov 1;24(21):5485. doi: ...
在既往接受过CDK4 /6抑制剂治疗的ABC进展患者中,阿贝西利+氟维司群显示出统计学上显著的PFS改善。 ▌参考文献: 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: Prim...
[8]Dickler MN,Tolaney SM,Rugo HS,et al.MONARCH 1,A Phase II Study of Abemaciclib,a CDK4 and CDK6 Inhibitor,as a Single Agent,in Patients with Refractory HR+/HER2-Metastatic Breast Cancer[published correction appears in Clin Cancer Res.2018 Nov 1;24(21):5485.doi:10.1158/1078-0432.CCR...