Difference between revisions of "Palbociclib (Ibrance)"
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==General information== | ==General information== | ||
| − | Class/mechanism: Cyclin-dependent kinase 4 and 6 inhibitor. Cyclin D1, CDK4, and CDK6 are downstream of signaling pathways which result in cellular proliferation. The use of palbociclib with antiestrogens was observed to increase growth arrest in estrogen receptor (ER)-positive breast cancer cell lines by decreasing retinoblastoma protein (Rb) phosphorylation, which resulted in reduced E2F expression and signaling. Palbociclib has been observed to cause cell cycle arrest between G1 to S phase of the cell cycle in ER-positive breast cancer cell lines.<ref name=insert>[http://labeling.pfizer.com/ShowLabeling.aspx?id=2191 Palbociclib (Ibrance) package insert]</ref><ref>[[Media:Palbociclib.pdf|Palbociclib (Ibrance) package insert (locally hosted backup)]]</ref><ref>[http://www.ibrance.com/ Ibrance manufacturer's website | + | Class/mechanism: Cyclin-dependent kinase 4 and 6 inhibitor. Cyclin D1, CDK4, and CDK6 are downstream of signaling pathways which result in cellular proliferation. The use of palbociclib with antiestrogens was observed to increase growth arrest in estrogen receptor (ER)-positive breast cancer cell lines by decreasing retinoblastoma protein (Rb) phosphorylation, which resulted in reduced E2F expression and signaling. Palbociclib has been observed to cause cell cycle arrest between G1 to S phase of the cell cycle in ER-positive breast cancer cell lines.<ref name=insert>[http://labeling.pfizer.com/ShowLabeling.aspx?id=2191 Palbociclib (Ibrance) package insert]</ref><ref>[[Media:Palbociclib.pdf|Palbociclib (Ibrance) package insert (locally hosted backup)]]</ref><ref>[http://www.ibrance.com/ Ibrance manufacturer's website]</ref> |
<br>Route: PO | <br>Route: PO | ||
<br>Extravasation: n/a | <br>Extravasation: n/a | ||
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==Also known as== | ==Also known as== | ||
| − | PD-0332991 | + | *'''Code name:''' PD-0332991 |
| + | *'''Brand name:''' Ibrance | ||
==References== | ==References== | ||
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[[Category:Drug index]] | [[Category:Drug index]] | ||
| − | |||
[[Category:Oral medications]] | [[Category:Oral medications]] | ||
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[[Category:Breast cancer medications]] | [[Category:Breast cancer medications]] | ||
[[Category:Drugs FDA approved in 2015]] | [[Category:Drugs FDA approved in 2015]] | ||
| + | [[Category:FDA approved drugs]] | ||
Revision as of 16:06, 8 October 2017
General information
Class/mechanism: Cyclin-dependent kinase 4 and 6 inhibitor. Cyclin D1, CDK4, and CDK6 are downstream of signaling pathways which result in cellular proliferation. The use of palbociclib with antiestrogens was observed to increase growth arrest in estrogen receptor (ER)-positive breast cancer cell lines by decreasing retinoblastoma protein (Rb) phosphorylation, which resulted in reduced E2F expression and signaling. Palbociclib has been observed to cause cell cycle arrest between G1 to S phase of the cell cycle in ER-positive breast cancer cell lines.[1][2][3]
Route: PO
Extravasation: n/a
For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the package insert.[1]
Diseases for which it is used
Patient drug information
- Palbociclib (Ibrance) package insert[1]
- Palbociclib (Ibrance) patient drug information (Chemocare)[4]
- Palbociclib (Ibrance) patient drug information (UpToDate)[5]
History of changes in FDA indication
- 2/3/2015: Accelerated FDA approval to be used "in combination with letrozole for the treatment of postmenopausal women with estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced breast cancer as initial endocrine-based therapy for their metastatic disease."
- 2/19/2016: FDA approval expanded "in combination with fulvestrant 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."
- 3/31/2017: FDA granted regular approval "for the treatment of hormone receptor (HR) positive, human epidermal growth factor receptor 2 (HER2) negative advanced or metastatic breast cancer in combination with an aromatase inhibitor as initial endocrine based therapy in postmenopausal women."[1]
Also known as
- Code name: PD-0332991
- Brand name: Ibrance