Ribociclib, a novel drug for targeted therapy of breast cancer
PENG Wen-xiu
DU Xiao-li
Abstract：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.
Keywords：ribociclibbreast cancerinhibitor of CDK4/6
Publication Date：2018-01-01
Online Publishing Date：2026-08-14(First online date of this platform, not the publication date of the document)
Pages：4( 8-11 )