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