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GIST Support International - Palbociclib Isethionate (PD-0332991
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Palbociclib Isethionate (PD-0332991)

This cell cycle inhibitor drug is under development and a clinical trial is expected soon.

For a dicussion of the anti-cancer potential of cell cycle inhibitors, see our page The Cell Cycle as a Drug Target by Gary Schwartz, MD.

 

Definition from NCI Drug Dictionary:
palbociclib isethionate --  An orally available cyclin-dependent kinase (CDK) inhibitor with 
potential antineoplastic activity. Palbociclib selectively inhibits cyclin-dependent kinase 4 (CDK4) and 6 (CDK6), thereby inhibiting retinoblastoma (Rb) protein phosphorylation early in the G1 phase 
leading to cell cycle arrest. 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.

 

Trial Expected Soon:

Efficacy and Safety of PD-0332991 in Patients With Advanced Gastrointestinal Stromal Tumors Refractory to Imatinib and Sunitinib (CYCLIGIST), NCT01907607



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