2015
DOI: 10.1007/s40265-015-0379-9
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Palbociclib: First Global Approval

Abstract: Palbociclib (Ibrance®) is an oral, reversible, selective, small-molecule inhibitor of cyclin-dependent kinases (CDK) 4 and CDK6 developed by Pfizer for the treatment of cancer. CDKs are important modulators of cell cycle entry and progression in response to growth signals, and inhibition of these kinases with palbociclib could enhance the activity of other anticancer drugs in tolerable regimens. Palbociclib, in combination with letrozole, was recently approved in the US for the first-line treatment of advanced… Show more

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Cited by 121 publications
(117 citation statements)
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“…It efficiently induces a G1 cell cycle arrest and subsequent cytostasis in vitro and in vivo [1][2][3][4][5]. Palbociclib has recently received FDA approval for treatment of estrogen receptor positive, human epidermal growth factor receptor 2 negative (ER+/HER2-) advanced breast cancer [6]. Many other clinical trials are ongoing, including one for treatment of retinoblastoma (Rb) proficient glioblastoma (GBM) (Clintrial.gov identifier: NCT01227434).…”
Section: Introductionmentioning
confidence: 99%
“…It efficiently induces a G1 cell cycle arrest and subsequent cytostasis in vitro and in vivo [1][2][3][4][5]. Palbociclib has recently received FDA approval for treatment of estrogen receptor positive, human epidermal growth factor receptor 2 negative (ER+/HER2-) advanced breast cancer [6]. Many other clinical trials are ongoing, including one for treatment of retinoblastoma (Rb) proficient glioblastoma (GBM) (Clintrial.gov identifier: NCT01227434).…”
Section: Introductionmentioning
confidence: 99%
“…12–14 Administration of one of the three CDK4/6 inhibitors with a strong CYP3A inhibitor (e.g. itraconazole) should be avoided, as well as administration with strong (e.g.…”
Section: Cdk4/6 Inhibitor Drug Interactionmentioning
confidence: 99%
“…The use of palbociclib against the cyclin-dependent kinases CDK4 and CDK6 has successfully been used in advanced breast cancer [58] and it is under evaluation in many other cancer types in phase II and III clinical trials [59]. In EC, Dosil et al [60] performed the first preclinical study to test the therapeutic potential of palbociclib; specifically, this was tested in the endometrial malignancies driven by Pten deficiency.…”
Section: Endometrial Cancer Pdx Modelsmentioning
confidence: 99%