立博昔利布是一種口服的小分子細胞周期蛋白依賴性激酶4/6抑制劑，通過抑制腫瘤細胞由G1期向S期轉換達到抑制腫瘤發(fā)展的目的。立博昔利布和來曲唑聯(lián)用已于2017年3月13日在美國獲批，作為激素受體陽性/人表皮生長因子2受體陰性的晚期和轉移性乳腺癌患者的治療藥物。臨床研究表明該藥對晚期和轉移性腫瘤有明顯的抑制作用；與來曲唑聯(lián)用較單獨使用來曲唑能顯著延長患者的無惡化生存期。該藥不良反應發(fā)生率較高，但是耐受性較好。介紹該藥的藥效學、藥動學、臨床觀察和不良反應研究進展。

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.