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。 Lebertixib is an orally administered small molecule cyclin-dependent kinase 4/6 inhibitor that inhibits tumor progression by inhibiting the conversion of tumor cells from G1 phase to S phase. The combination of lexalolubicin and letrozole was approved in the United States on March 13, 2017 as a treatment for patients with hormone receptor-positive / human epidermal growth factor 2 receptor-negative patients with advanced and metastatic breast cancer. Clinical studies have shown that the drug has a significant inhibitory effect on advanced and metastatic tumors; the combination of letrozole and letrozole alone significantly prolongs the progression-free survival of patients. The drug has a higher incidence of adverse reactions, but better tolerated. The pharmacodynamics, pharmacokinetics, clinical observation and adverse reactions of the drug are introduced.