Zangardi Mark L, Spring Laura M, Blouin Gayle C, Bardia Aditya
a Ambulatory Oncology, Department of Pharmacy , Massachusetts General Hospital , Boston , MA , USA.
b Department of Oncology , Massachusetts General Hospital, Harvard Medical School , Boston , MA , USA.
Expert Rev Clin Pharmacol. 2017 Nov;10(11):1169-1176. doi: 10.1080/17512433.2017.1376653. Epub 2017 Sep 18.
The introduction of CDK4/6 inhibitors, such as ribociclib, has changed the treatment landscape for post-menopausal women with HR+/HER2- advanced or metastatic breast cancer. As first-line treatment of HR+/HER2- MBC, the addition of a CDK4/6 inhibitor to an aromatase inhibitor improves progression-free survival compared to an aromatase inhibitor alone. Areas covered: In this drug profile, we review the current market for HR+/HER2- MBC, as well as the characteristics, mechanism, pharmacology, pharmacodynamics, pharmacokinetics, metabolism, clinical efficacy, toxicities, monitoring, and dosing modification of the CDK4/6 inhibitor ribociclib. Expert commentary: CDK4/6 inhibitors, such as ribociclib, improve outcomes in post-menopausal women with HR+/HER2- MBC. The most common toxicity of ribociclib is neutropenia, which is generally not complicated and can be managed with dose modification and/or supportive care measures. Additional research will help better define the optimal clinical use of ribociclib.
诸如瑞博西尼等细胞周期蛋白依赖性激酶4/6（CDK4/6）抑制剂的引入，改变了激素受体阳性/人表皮生长因子受体2阴性（HR+/HER2-）晚期或转移性乳腺癌绝经后女性的治疗格局。作为HR+/HER2-转移性乳腺癌（MBC）的一线治疗，与单独使用芳香化酶抑制剂相比，在芳香化酶抑制剂基础上加用CDK4/6抑制剂可改善无进展生存期。涵盖领域：在本药物简介中，我们综述了HR+/HER2-MBC的当前市场情况，以及CDK4/6抑制剂瑞博西尼的特性、作用机制、药理学、药效学、药代动力学、代谢、临床疗效、毒性、监测及剂量调整。专家评论：诸如瑞博西尼等CDK4/6抑制剂可改善HR+/HER2-MBC绝经后女性的治疗结局。瑞博西尼最常见的毒性是中性粒细胞减少，一般并不复杂，可通过剂量调整和/或支持性护理措施进行处理。更多研究将有助于更好地明确瑞博西尼的最佳临床应用。
