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乳腺癌靶向治疗新药ribociclib
乳腺癌靶向治疗新药ribociclib
彭文绣,杜小莉

中国医学科学院北京协和医学院北京协和医院药剂科,北京 100730
Ribociclib, a novel drug for targeted therapy of breast cancer
(Department of Pharmacy, Peking Union Medical College Hospital, Chinese Academy of Medical Sciences, Beijing 100730, China)

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起始页:8

摘要:[摘要] Ribociclib(商品名:Kisqali)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。

关键词:[关键词] ribociclib;乳腺癌;CDK4/6抑制剂

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Abstract:[Abstract] Ribociclib, with the brand name of Kisqali, 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.

Key words:[Key words] ribociclib; breast cancer; inhibitor of CDK4/6

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