Breast cancer is the most frequently diagnosed neoplasm in the world. It can be classified into four main subtypes, each of them showing differences in the expression of hormone receptor (HR), human epidermal growth factor receptor 2 (HER2), and in cell metabolism. Since 2015, when The U.S. Food and Drug Administration (FDA) approved the first cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitor that regulates the cell cycle, treatment of HR+/HER2− BC has become much more effective. Currently, palbociclib, ribociclib, and abemaciclib are more often used both in combination with endocrine therapy as well as in monotherapy. Their application has been extensively verified in many clinical trials such as PALOMA-1,2,3, MONALEESA-1,2,3,7, and MONARCH-1,2,3, which allowed the verification of differences in their effectiveness, dosage, and adverse effects. Subsequent studies, MonarchE and NATALEE, examined the role of these inhibitors as adjuvant therapy, as well as at verifying their safety. Moreover, dalpiciclib is being investigated in HR+/HER2− BC treatment. This article will summarize clinical efficacy, recommendations, and differences in toxicity profile between palbociclib, ribociclib, and abemaciclib and will also discuss the possibility of using dalpiciclib in the treatment of breast cancer.
乳腺癌是全球范围内最常被诊断出的恶性肿瘤。根据激素受体（HR）、人表皮生长因子受体2（HER2）的表达情况及细胞代谢特征，可将其分为四种主要亚型。自2015年美国食品药品监督管理局（FDA）批准首个用于调控细胞周期的细胞周期蛋白依赖性激酶4和6（CDK4/6）抑制剂以来，HR+/HER2-型乳腺癌的治疗效果显著提升。目前，帕博西尼、瑞博西尼和阿贝西利更常与内分泌治疗联合使用或作为单药治疗。这些药物的应用已通过PALOMA-1、2、3，MONALEESA-1、2、3、7及MONARCH-1、2、3等多项临床试验得到广泛验证，从而明确了它们在疗效、剂量和不良反应方面的差异。后续的MonarchE和NATALEE研究进一步探讨了这些抑制剂作为辅助治疗的作用及其安全性验证。此外，达尔西利在HR+/HER2-型乳腺癌治疗中的应用也正在研究中。本文将总结帕博西尼、瑞博西尼和阿贝西利的临床疗效、使用建议及毒性特征差异，并探讨达尔西利在乳腺癌治疗中的应用前景。
CDK4/6 as a Therapeutic Target in HR+/HER2− Breast Cancer Cells—Current Treatment Status
肿瘤(癌症)患者之家