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Ribociclib(商品名:Kisqali(R)是一类新型靶向小分子药物,可选择性抑制细胞周期蛋白依赖性激酶4/6 (CDK4/6)的活性,阻断成视网膜母细胞瘤蛋白的磷酸化过程,减少乳腺癌细胞系增殖而发挥抗肿瘤作用.临床研究证实,与单用来曲唑治疗相比,ribociclib与来曲唑联合用药能延长患者无进展生存期.因此,该药获得FDA的突破性药物认定并于2017年3月13日批准上市.Ribociclib可与芳香酶抑制剂联合作为初始内分泌类治疗方案,用于绝经后激素受体阳性、人类表皮生长因子受体-2阴性的晚期或转移性乳腺癌女性患者.本文对ribociclib的作用机制、药动学、临床评价、药物相互作用和安全性等进行归纳总结.“,”Ribociclib,with the brand name of Kisqali(R),is a targeted small molecule drug which selectively inhibits cyclin-dependent kinases 4 and 6(CDK4/6) activity.The inhibition of CDK results in the dephosphorylation of retinoblastoma protein which depresses the transcription of multiple genes required for cell cycle progression.Clinical studies showed that,compared with letrozole,the progression-free-survival of patients was extended after treatment with ribociclib combined with letrozole.Therefore,the drug,which was regarded as a breakthrough product,was approved by the US FDA on March 13th,2017.Ribociclib is indicated in combination with an aromatase inhibitor as initial endocrine-based therapy for the treatment of postmenopausal women with hormone receptor (HR)-positive,human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancers.In this article,the mechanism,pharmacokinetics,clinical evaluation,drug interaction and safety of ribociclib were reviewed.