立博昔利布是一种口服的小分子细胞周期蛋白依赖性激酶4/6抑制剂，通过抑制肿瘤细胞由G1期向S期转换达到抑制肿瘤发展的目的。立博昔利布和来曲唑联用已于2017年3月13日在美国获批，作为激素受体阳性/人表皮生长因子2受体阴性的晚期和转移性乳腺癌患者的治疗药物。临床研究表明该药对晚期和转移性肿瘤有明显的抑制作用；与来曲唑联用较单独使用来曲唑能显著延长患者的无恶化生存期。该药不良反应发生率较高，但是耐受性较好。介绍该药的药效学、药动学、临床观察和不良反应研究进展。

Ribociclib is an oral small molecule cyclindependent kinase 4/6 inhibitor, which inhibits tumor progression by inhibiting the conversion of tumor cells from G1 phase to S phase. The combination of ribociclib and letrozole was approved in the United States on March 13, 2017 as a treatment for HR+/HER2- advanced and metastatic breast cancer patients. Clinical results showed that the drug on advanced and metastatic tumors had a significant inhibitory effect and could extend the survival of patients without deterioration compared with using letrozole alone. The incidence of adverse drug reactions is higher, but the tolerance is better. This article focuses on pharmacodynamics, pharmacokinetic, clinical results and adverse effects of this drug.