Alpelisib in the treatment of metastatic HR+ breast cancer with PIK3CA mutations

Since the US FDA approval of everolimus/exemestane in July 2012, and of the first CDK 4/6 inhibitor, palbociclib, combined with endocrine treatment in February 2015, a third class of therapeutic compounds, the PI3K inhibitors, has been introduced to the arsenal of targeted therapies overcoming endoc...

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Bibliographic Details
Main Authors: Mavratzas, Athanasios (Author) , Marmé, Frederik (Author)
Format: Article (Journal)
Language:English
Published: 23 Sep 2020
In: Future oncology
Year: 2020, Volume: 17, Issue: 1, Pages: 13-36
ISSN:1744-8301
DOI:10.2217/fon-2020-0464
Online Access:Verlag, lizenzpflichtig, Volltext: https://doi.org/10.2217/fon-2020-0464
Verlag, lizenzpflichtig, Volltext: https://www.futuremedicine.com/doi/10.2217/fon-2020-0464
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Author Notes:Athanasios Mavratzas, Frederik Marmé
Description
Summary:Since the US FDA approval of everolimus/exemestane in July 2012, and of the first CDK 4/6 inhibitor, palbociclib, combined with endocrine treatment in February 2015, a third class of therapeutic compounds, the PI3K inhibitors, has been introduced to the arsenal of targeted therapies overcoming endocrine resistance in hormone receptor-positive metastatic breast cancer. Alpelisib (PIQRAY®) is the first of these novel agents yielding promising clinical results, giving an impetus to further development of tailored endocrine anticancer treatments. Herein, we review its pharmacodynamic and pharmacokinetic properties, safety and efficacy data, as well as Phase III SOLAR-1 trial, prompting FDA approval of alpelisib in hormone receptor-positive metastatic breast cancer harboring PIK3CA mutations. Furthermore, implications for clinical use and current research will also be discussed.
Item Description:Gesehen am 12.05.2021
Physical Description:Online Resource
ISSN:1744-8301
DOI:10.2217/fon-2020-0464