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Synonyms: Ibrance® | PD-0332991 | PD0332991
palbociclib is an approved drug (FDA (2015), EMA (2016))
Compound class: Synthetic organic
Comment: Palbociclib is a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6 [6-7,14]. This kinase inhibitor has anti-tumour activity in several tumour models [6-7,9,15-16].
The pharmaceutical formulation contains palbociclib isethionate (PubChem CID 11478676).
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
View more information in the IUPHAR Pharmacology Education Project: palbociclib
|No information available.|
|Summary of Clinical Use|
|In August 2014 the drug's developer, Pfizer, announced the start of a multi-center, open-label expanded access program (EAP) in the United States. Through this program, palbociclib is being made available for use in combination with letrozole (an aromatase inhibitor) for post-menopausal women with hormone receptor positive (HR+), human epidermal growth factor receptor 2 negative (HER2-) advanced breast cancer for whom letrozole is considered appropriate therapy. This EAP is registered as clinical trial NCT02142868.
In February 2015 the US FDA approved palbociclib for the treatment of postmenopausal women with advanced (metastatic) breast cancer (in combination with letrozole as described above [1,5,8,17]). In early 2016, the FDA expanded use further by approving palbociclib in combination with fulvestrant (an estrogen receptor antagonist) for the treatment of women with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer with disease progression following endocrine therapy .
Palbociclib is being tested in many clinical trials to assess effectiveness against several other types of cancer. To view the current list of trials link to ClinicalTrials.gov.
|Mechanism Of Action and Pharmacodynamic Effects|
|The cyclin D-CDK4/6 (CDK-4/6:INK4:Rb) pathway is key to regulating cell growth in many types of human cancer [2,10-11], such as genetic subtypes of non-small cell lung cancer (NSCLC, [3,10,18], melanoma, Mantle cell lymphoma (MCL), and ovarian and breast cancers [3-4]. Inhibiting this pathway prevents cell cycle transition from G1 to S phase, induces cell senescence and in some cases results in apoptosis .|
For extended ADME data see the following:
Electronic Medicines Compendium (eMC)
European Medicines Agency (EMA)