对于存在这样的差异,考虑可能原因如下:第一,不同CDK4/6抑制剂在药物作用机制上还是有所差异的,阿贝西利对CDK4的抑制比对CDK6的抑制能力更强,而哌柏西利则对两者的抑制强度相当,并且阿贝西利对CDK9也有一定的抑制作用[53]。药物作用机制的不同是否会带来疗效和...
3 Recently, cyclin-dependent kinase (CDK) 4/6 inhibitors have been changing practice in advanced HR-positive breast cancer, with 3 agents (palbociclib [Ibrance], ribociclib [Kisqali], and abemaciclib [Verzenio]) having now FDA-approved indications for use with ET in the first-line setting.4-...
[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 ...
Regarding the advances we’re making in targeted therapies, we have a newly approved AKT inhibitor, capivasertib, that’s highly active. Patients are eligible [to receive this agent] if they have activating mutations in PIK3CA, but also in...
未来还需更多高质量的研究继续进行晚期乳腺癌治疗的探索,期待国产口服 SARM EG017 能够延续甚至超越现有类似药物,为乳腺癌患者治疗的临床实践提供更多疗效优秀安全可控的靶向 AR 内分泌治疗药物,为 CDK4/6i 后治疗再次添砖加瓦。 参考...
et al. CDK4/6 inhibitor treatment for patients with hormone receptor-positive, HER2-negative, advanced or metastatic breast cancer: a US Food and Drug Administration pooled analysis. Lancet Oncol. 21, 250–260 (2020). Article CAS PubMed Google Scholar Wedam, S. et al. FDA approval ...
[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...
The multi-faceted experimental and computational approaches described here therefore uncover under-appreciated differences in CDK4/6 inhibitor activities with potential importance in treating human patients.doi:10.1101/211680Marc HafnerCaitlin E. Mills
Three FDA approved CDK4/6 inhibitors, Palbociclib, Ribociclib and Abemaciclib, have been used as targeted cancer therapeutic agents to benefit patients with endocrine therapy-resistant breast cancer and other types of cancer, prolonging their survival. However, the clinical application of these ...
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...