Palbociclib

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Information about Palbociclib

Palbociclib is a unique cyclin-dependent kinase inhibitor that is used in combination with aromatase inhibitors in the treatment of postmenopausal women with metastatic breast cancer.

Liver safety of Palbociclib

Palbociclib is associated with transient and usually mild elevations in serum aminotransferase during therapy, but has yet to be linked to cases of clinically apparent acute liver injury.   

Mechanism of action of Palbociclib

Palbociclib (pal" boe sye' klib) is an orally available, specific inhibitor of cyclin-dependent kinases that is used in combination with aromatase inhibitors in the therapy of postmenopausal women with metastatic breast cancer that is positive for the estrogen receptor (ER+), but negative for human epidermal growth factor receptor 2 (HER2-).  The cyclin kinases 4 and 6 regulate the cellular transition from the G1 to the S phase of the cell cycle.  Inhibition of this transition blocks the progression of the cell cycle and results in growth arrest in rapidly dividing cells.  The addition of palbociclib to letrozole or fulvestrant (aromatase inhibitors) therapy of metastatic breast cancer (ER+, HER2-) in postmenopausal women was associated with a prolongation of disease free survival. 

FDA approval information for Palbociclib

Palbociclib received accelerated approval for use in the United States in 2015, and it is still under close evaluation for its long term safety and efficacy. 

Dosage and administration for Palbociclib

Palbociclib is available in capsules of 75, 100 and 125 mg and the typical maintenance dose is 125 mg once daily in 21 day cycles every 28 days indefinitely or until there is disease progression. 

Side effects of Palbociclib

Common side effects include fatigue, nausea, diarrhea, anorexia, neutropenia, fever, anemia, thrombocytopenia, epistasis, peripheral neuropathy and pulmonary embolism. Severe adverse events include neutropenia fever and sepsis

 


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