Profile of buparlisib and its potential in the treatment of breast cancer: evidence to date

Carmen Criscitiello, Giulia Viale, Giuseppe Curigliano, Aron Goldhirsch European Institute of Oncology, Milano, Italy Abstract: Alteration of the phosphatidylinositol 3-kinase (PI3K)/AKT/mammalian target of rapamycin signaling pathway is key for the growth and survival of...

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Autores principales:	Criscitiello C, Viale G, Curigliano G, Goldhirsch A
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2018
Materias:	buparlisib breast cancer PI3K Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282
Acceso en línea:	https://doaj.org/article/d5bcc36067914069a34e9071aacf3d50
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spelling	oai:doaj.org-article:d5bcc36067914069a34e9071aacf3d502021-12-02T09:42:29ZProfile of buparlisib and its potential in the treatment of breast cancer: evidence to date1179-1314https://doaj.org/article/d5bcc36067914069a34e9071aacf3d502018-01-01T00:00:00Zhttps://www.dovepress.com/profile-of-buparlisib-and-its-potential-in-the-treatment-of-breast-can-peer-reviewed-article-BCTThttps://doaj.org/toc/1179-1314Carmen Criscitiello, Giulia Viale, Giuseppe Curigliano, Aron Goldhirsch European Institute of Oncology, Milano, Italy Abstract: Alteration of the phosphatidylinositol 3-kinase (PI3K)/AKT/mammalian target of rapamycin signaling pathway is key for the growth and survival of several cancers, including breast cancer. In addition, dysregulation of PI3K signaling may contribute to resistance to several anticancer agents. PI3K inhibitors may, therefore, be effective as antineoplastic therapy. Buparlisib is a potent and highly specific oral inhibitor of the pan-class I PI3K family. Buparlisib specifically inhibits class I PIK3 in the PI3K/AKT kinase signaling pathway in an ATP-competitive manner, thus inhibiting the production of the secondary messenger phosphatidylinositol (3,4,5)-trisphosphate and activation of the PI3K signaling pathway. This may induce inhibition of tumor cell growth and survival in susceptible tumor cell populations. Buparlisib is currently under investigation in patients with a variety of solid tumors, including breast cancer. Buparlisib has been validated as a promising anticancer agent, and tremendous efforts have been taken to develop it. However, buparlisib monotherapy has resulted in humble benefit so far. Results from studies combining buparlisib with different anticancer agents – namely, endocrine therapy, anti-HER2 therapy, and chemotherapy – have showed variable efficacy with consistent substantial toxicity. Keywords: buparlisib, breast cancer, PI3K Criscitiello CViale GCurigliano GGoldhirsch ADove Medical Pressarticlebuparlisib breast cancer PI3KNeoplasms. Tumors. Oncology. Including cancer and carcinogensRC254-282ENBreast Cancer: Targets and Therapy, Vol Volume 10, Pp 23-29 (2018)
institution	DOAJ
collection	DOAJ
language	EN
topic	buparlisib breast cancer PI3K Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282
spellingShingle	buparlisib breast cancer PI3K Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282 Criscitiello C Viale G Curigliano G Goldhirsch A Profile of buparlisib and its potential in the treatment of breast cancer: evidence to date
description	Carmen Criscitiello, Giulia Viale, Giuseppe Curigliano, Aron Goldhirsch European Institute of Oncology, Milano, Italy Abstract: Alteration of the phosphatidylinositol 3-kinase (PI3K)/AKT/mammalian target of rapamycin signaling pathway is key for the growth and survival of several cancers, including breast cancer. In addition, dysregulation of PI3K signaling may contribute to resistance to several anticancer agents. PI3K inhibitors may, therefore, be effective as antineoplastic therapy. Buparlisib is a potent and highly specific oral inhibitor of the pan-class I PI3K family. Buparlisib specifically inhibits class I PIK3 in the PI3K/AKT kinase signaling pathway in an ATP-competitive manner, thus inhibiting the production of the secondary messenger phosphatidylinositol (3,4,5)-trisphosphate and activation of the PI3K signaling pathway. This may induce inhibition of tumor cell growth and survival in susceptible tumor cell populations. Buparlisib is currently under investigation in patients with a variety of solid tumors, including breast cancer. Buparlisib has been validated as a promising anticancer agent, and tremendous efforts have been taken to develop it. However, buparlisib monotherapy has resulted in humble benefit so far. Results from studies combining buparlisib with different anticancer agents – namely, endocrine therapy, anti-HER2 therapy, and chemotherapy – have showed variable efficacy with consistent substantial toxicity. Keywords: buparlisib, breast cancer, PI3K
format	article
author	Criscitiello C Viale G Curigliano G Goldhirsch A
author_facet	Criscitiello C Viale G Curigliano G Goldhirsch A
author_sort	Criscitiello C
title	Profile of buparlisib and its potential in the treatment of breast cancer: evidence to date
title_short	Profile of buparlisib and its potential in the treatment of breast cancer: evidence to date
title_full	Profile of buparlisib and its potential in the treatment of breast cancer: evidence to date
title_fullStr	Profile of buparlisib and its potential in the treatment of breast cancer: evidence to date
title_full_unstemmed	Profile of buparlisib and its potential in the treatment of breast cancer: evidence to date
title_sort	profile of buparlisib and its potential in the treatment of breast cancer: evidence to date
publisher	Dove Medical Press
publishDate	2018
url	https://doaj.org/article/d5bcc36067914069a34e9071aacf3d50
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Profile of buparlisib and its potential in the treatment of breast cancer: evidence to date

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