PI3Kinase Inhibition in Hormone Receptor-Positive Breast Cancer

Derangement of the phosphatidylinositol-3 kinase (PI3K) pathway is implicated in several subtypes of breast cancers. Mutation or upregulation of PI3K enhances cancer cells’ survival, proliferation, and ability to metastasize, making it an attractive molecular target for systemic therapy. PI3K has fo...

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Autores principales: Ajay Dhakal, Luna Acharya, Ruth O’Regan, Shipra Gandhi, Carla Falkson
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Lenguaje:EN
Publicado: MDPI AG 2021
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Acceso en línea:https://doaj.org/article/de52808cef934de585708bda5de0bea6
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spelling oai:doaj.org-article:de52808cef934de585708bda5de0bea62021-11-11T17:18:00ZPI3Kinase Inhibition in Hormone Receptor-Positive Breast Cancer10.3390/ijms2221118781422-00671661-6596https://doaj.org/article/de52808cef934de585708bda5de0bea62021-11-01T00:00:00Zhttps://www.mdpi.com/1422-0067/22/21/11878https://doaj.org/toc/1661-6596https://doaj.org/toc/1422-0067Derangement of the phosphatidylinositol-3 kinase (PI3K) pathway is implicated in several subtypes of breast cancers. Mutation or upregulation of PI3K enhances cancer cells’ survival, proliferation, and ability to metastasize, making it an attractive molecular target for systemic therapy. PI3K has four isoforms, and several drugs targeting individual isoforms or pan-PI3K have been or are currently being investigated in clinical trials. However, the search for an effective PI3K inhibitor with a robust therapeutic effect and reasonable safety profile for breast cancer treatment remains elusive. This review focuses on the recently completed and ongoing clinical trials involving PI3K inhibitors as mono- or combination therapy in breast cancer. We review the salient findings of clinical trials, the therapeutic efficacy of PI3K inhibitors, and reported adverse effects leading to treatment discontinuation. Lastly, we discuss the challenges and potential opportunities associated with adopting PI3K inhibitors in the clinic.Ajay DhakalLuna AcharyaRuth O’ReganShipra GandhiCarla FalksonMDPI AGarticlePI3Kinase inhibitorhormone receptor positive breast cancerbreast cancerBiology (General)QH301-705.5ChemistryQD1-999ENInternational Journal of Molecular Sciences, Vol 22, Iss 11878, p 11878 (2021)
institution DOAJ
collection DOAJ
language EN
topic PI3Kinase inhibitor
hormone receptor positive breast cancer
breast cancer
Biology (General)
QH301-705.5
Chemistry
QD1-999
spellingShingle PI3Kinase inhibitor
hormone receptor positive breast cancer
breast cancer
Biology (General)
QH301-705.5
Chemistry
QD1-999
Ajay Dhakal
Luna Acharya
Ruth O’Regan
Shipra Gandhi
Carla Falkson
PI3Kinase Inhibition in Hormone Receptor-Positive Breast Cancer
description Derangement of the phosphatidylinositol-3 kinase (PI3K) pathway is implicated in several subtypes of breast cancers. Mutation or upregulation of PI3K enhances cancer cells’ survival, proliferation, and ability to metastasize, making it an attractive molecular target for systemic therapy. PI3K has four isoforms, and several drugs targeting individual isoforms or pan-PI3K have been or are currently being investigated in clinical trials. However, the search for an effective PI3K inhibitor with a robust therapeutic effect and reasonable safety profile for breast cancer treatment remains elusive. This review focuses on the recently completed and ongoing clinical trials involving PI3K inhibitors as mono- or combination therapy in breast cancer. We review the salient findings of clinical trials, the therapeutic efficacy of PI3K inhibitors, and reported adverse effects leading to treatment discontinuation. Lastly, we discuss the challenges and potential opportunities associated with adopting PI3K inhibitors in the clinic.
format article
author Ajay Dhakal
Luna Acharya
Ruth O’Regan
Shipra Gandhi
Carla Falkson
author_facet Ajay Dhakal
Luna Acharya
Ruth O’Regan
Shipra Gandhi
Carla Falkson
author_sort Ajay Dhakal
title PI3Kinase Inhibition in Hormone Receptor-Positive Breast Cancer
title_short PI3Kinase Inhibition in Hormone Receptor-Positive Breast Cancer
title_full PI3Kinase Inhibition in Hormone Receptor-Positive Breast Cancer
title_fullStr PI3Kinase Inhibition in Hormone Receptor-Positive Breast Cancer
title_full_unstemmed PI3Kinase Inhibition in Hormone Receptor-Positive Breast Cancer
title_sort pi3kinase inhibition in hormone receptor-positive breast cancer
publisher MDPI AG
publishDate 2021
url https://doaj.org/article/de52808cef934de585708bda5de0bea6
work_keys_str_mv AT ajaydhakal pi3kinaseinhibitioninhormonereceptorpositivebreastcancer
AT lunaacharya pi3kinaseinhibitioninhormonereceptorpositivebreastcancer
AT ruthoregan pi3kinaseinhibitioninhormonereceptorpositivebreastcancer
AT shipragandhi pi3kinaseinhibitioninhormonereceptorpositivebreastcancer
AT carlafalkson pi3kinaseinhibitioninhormonereceptorpositivebreastcancer
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