Difference between revisions of "Palbociclib (Ibrance)"
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(Created page with "==Mechanism of action== Orally bioavailable cyclin-dependent kinase 4/6 inhibitor. ==Preliminary data== # Vaughn DJ, Hwang W, Lal P, Rosen MA, Gallagher M, O'Dwyer PJ. Phase ...") |
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| − | == | + | ==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://www.ibrance.com/files/USPI%20-%20Ibrance%20-%20palbociclib%20-%20capsules%20-%20Feb%202015.pdf 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><ref>Vaughn DJ, Hwang W, Lal P, Rosen MA, Gallagher M, O'Dwyer PJ. Phase 2 trial of the cyclin-dependent kinase 4/6 inhibitor palbociclib in patients with retinoblastoma protein-expressing germ cell tumors. Cancer. 2014 Dec 18. [Epub ahead of print] [http://onlinelibrary.wiley.com/doi/10.1002/cncr.29213/full link to original article] [http://www.ncbi.nlm.nih.gov/pubmed/25522918 PubMed]</ref> | |
| + | <br>Route: PO | ||
| + | <br>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 [http://www.thomsonhc.com/home/dispatch Micromedex], [http://online.lexi.com/ Lexicomp], [http://www.utdol.com/online/content/search.do UpToDate (courtesy of Lexicomp)], or the package insert.<ref name="insert"></ref> | |
| − | + | ||
| + | ==Diseases for which it is used== | ||
| + | *[[Breast cancer]] | ||
| + | |||
| + | ==Patient drug information== | ||
| + | *[http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207103s000lbl.pdf Palbociclib (Ibrance) package insert]<ref name="insert"></ref> | ||
| + | |||
| + | ==History of changes in FDA indication== | ||
| + | *2/3/2015: [http://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm432886.htm Accelerated FDA approval] to be used "in combination with [[Letrozole (Femara) | 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." | ||
| + | |||
| + | ==Also known as== | ||
| + | PD-0332991 | ||
| + | |||
| + | ==References== | ||
| + | <references/> | ||
[[Category:Drug index]] | [[Category:Drug index]] | ||
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[[Category:Oral chemotherapy]] | [[Category:Oral chemotherapy]] | ||
| + | [[Category:Enzyme inhibitors]] | ||
[[Category:Kinase inhibitors]] | [[Category:Kinase inhibitors]] | ||
[[Category:CDK inhibitors]] | [[Category:CDK inhibitors]] | ||
| − | [[Category: | + | [[Category:Breast cancer medications]] |
| + | [[Category:Drugs FDA approved in 2015]] | ||
Revision as of 15:03, 4 February 2015
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][4]
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
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."
Also known as
PD-0332991
References
- ↑ 1.0 1.1 1.2 Palbociclib (Ibrance) package insert
- ↑ Palbociclib (Ibrance) package insert (locally hosted backup)
- ↑ Ibrance manufacturer's website
- ↑ Vaughn DJ, Hwang W, Lal P, Rosen MA, Gallagher M, O'Dwyer PJ. Phase 2 trial of the cyclin-dependent kinase 4/6 inhibitor palbociclib in patients with retinoblastoma protein-expressing germ cell tumors. Cancer. 2014 Dec 18. [Epub ahead of print] link to original article PubMed