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随着肿瘤分子生物学研究的进展，晚期乳腺癌的临床治疗理念逐渐趋向精准化。激素受体(HR)阳性人表皮生长因子受体2(HER-2)阴性乳腺癌在所有乳腺癌中占比>70%，探讨新的治疗策略以突破此类患者面临的传统治疗瓶颈意义重大。HR阳性HER-2阴性乳腺癌的靶向治疗起步较晚，自首个CDK4/6抑制剂哌柏西利于2015年进入临床应用于治疗HR阳性HER-2阴性晚期乳腺癌患者之后，这类分子靶向药物的应用显著改变了HR阳性HER-2阴性晚期乳腺癌的临床治疗模式，患者生存预后也随之获得突破性改善。文章从基础药理机制出发，分析了现有的研究数据，就将来如何在临床实现精准化用药以及未来更广泛的应用前景提出见解。“,”With the progress of tumor molecular biology research, the clinical treatment concept of advanced breast cancer gradually tends to be accurate. Hormone receptor (HR) positive and human epidermal growth factor receptor 2 (HER-2) negative breast cancer accounts for more than 70% of all breast cancers, and it is of great significance to explore new treatment strategies to break through the bottleneck of traditional treatment faced by the patient population. Targeted therapy for this type of breast cancer started relatively late. After the first cyclin-dependent kinase (CDK) 4/6 inhibitor Palbociclib entered the clinical application for HR positive and HER-2 negative advanced breast cancer patients in 2015, the clinical treatment pattern of HR positive and HER-2 negative advanced breast cancer has been changed significantly, with a consequent breakthrough improvement in patients′ survival prognosis. Based on the basic pharmacological mechanism, the author analyzes the existing research data and puts forward opinions on how to achieve precise medication in clinical practice and wider application prospects in the future.