Inhibiting the PI3K signaling pathway: buparlisib as a new targeted option in breast carcinoma.
Aberrations in the PI3K signaling pathway are frequently observed in patients with breast cancer. Because of that, PI3K inhibitors are attractive options for the treatment of breast cancer because PI3K is the most proximal component of the pathway other than receptor tyrosine kinases. Buparlisib is a potent and highly specific oral pan-class I PI3K inhibitor, which is currently under investigation in patients with breast cancer. In this article, we describe the PI3K signaling pathway, the prognostic value of PI3K pathway mutations, as well as the mechanism of action of buparlisib. Lastly, we discuss preliminary results of preclinical and clinical studies showing the efficacy and safety profile of this agent in breast cancer patients.
Breast Cancer Programme, Centro Integral Oncológico Clara Campal, Oña, 10, 28050, Madrid, Spain. lestevez@hmhospitales.com.
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Estévez
Pathology Department, Hospital Universitario Fundación Alcorcón, Budapest, 1, 28922, Alcorcón, Madrid, Spain.
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García
Clinical Research Programme, Spanish National Cancer Research Centre (CNIO), Melchor Fernández Almagro, 3, 28029, Madrid, Spain.
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Hidalgo
D000631:Aminopyridines / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000378:metabolism / Q000473:pathology*; D005260:Female; D006801:Humans; D051379:Mice; D058990:Molecular Targeted Therapy / Q000379:methods*; D009025:Morpholines / Q000494:pharmacology*; D019869:Phosphatidylinositol 3-Kinases / Q000378:metabolism*; D015398:Signal Transduction / Q000187:drug effects
D000631:Aminopyridines; D000970:Antineoplastic Agents; D009025:Morpholines; C571178:NVP-BKM120; D019869:Phosphatidylinositol 3-Kinases
Breast cancer; Buparlisib; PI3K inhibitor; PI3KCA; Targeted therapy