药物总结
Palbociclib (PD-0332991)
Palbociclib is an orally available cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. Palbociclibselectively inhibits cyclin-dependent kinase 4 (CDK4) and 6 (CDK6), thereby inhibiting retinoblastoma (Rb) protein phosphorylation（Ser780） early in the G1 phase leading to cell cycle arrest.导致减低E2F表达和信号和阻止增加生长This suppresses DNA replication and decreases tumor cell proliferation. CDK4 and 6 are serine/threonine kinases that are upregulated in many tumor cell types and play a key role in the regulation of cell cycle progression.
US.FDA has approved the drug market with the new name ibrance in the USA and Pfizer is going to present the application to EU(European Union) in September this year.
BMS754807
Bazedoxifeneacetate醋酸巴多昔芬