科研之友
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摘要
Palbociclib is an investigational, oral and selective inhibitor of the cyclin-dependent kinases (CDKs) 4 and 6. CDK4 and CDK6 interact with cyclin D to enable tumor cell progression during the G 1 phase of the cell cycle. The cyclin D/CDK4 pathway is aberrantly regulated in the majority of cancers, leading to an increase in the number of cells entering the cell cycle and promoting tumor growth. Inhibition of aberrant cell cycle entry is therefore a major clinical target for anticancer drug development. In preclinical studies, palbociclib demonstrated effective CDK4/6 inhibition, arresting a wide variety of cancer cell types in the G 1 phase and inhibiting cellular proliferation both in vitro and in vivo. Phase I studies were conducted to determine the pharmacokinetic profile of the drug in humans and to assess efficacy and dosing schedules for progression to phase II studies. Palbociclib was recently granted breakthrough therapy designation by the FDA following the presentation of data from a phase II evaluation of the drug in patients with breast cancer demonstrating a marked improvement in progression-free survival. The drug is currently under phase II/III clinical evaluation as a single agent or in combination for various cancers.
- 出版日期2013-11
