Profile of neratinib and its potential in the treatment of breast cancer

Katharina Feldinger,1 Anthony Kong,2 1Department of Oncology, The Weatherall Institute of Molecular Medicine, University of Oxford, Oxford, 2The Robert Aitkin Institute, School of Cancer Sciences, University of Birmingham, Birmingham, UK Abstract: The HER (ErbB) receptor tyrosine kinase receptors a...

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Main Authors: Feldinger K, Kong A
Format: Article
Language:English
Published: Dove Medical Press 2015-06-01
Series:Breast Cancer: Targets and Therapy
Online Access:http://www.dovepress.com/profile-of-neratinib-and-its-potential-in-the-treatment-of-breast-canc-peer-reviewed-article-BCTT
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author Feldinger K
Kong A
author_facet Feldinger K
Kong A
author_sort Feldinger K
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description Katharina Feldinger,1 Anthony Kong,2 1Department of Oncology, The Weatherall Institute of Molecular Medicine, University of Oxford, Oxford, 2The Robert Aitkin Institute, School of Cancer Sciences, University of Birmingham, Birmingham, UK Abstract: The HER (ErbB) receptor tyrosine kinase receptors are implicated in many cancers and several anti-HER treatments are now approved. In recent years, a new group of compounds that bind irreversibly to the adenosine triphosphate binding pocket of HER receptors have been developed. One of these compounds, neratinib, has passed preclinical phases and is currently undergoing various clinical trials. This manuscript reviews the preclinical as well as clinical data on neratinib. As a pan-HER inhibitor, this irreversible tyrosine kinase inhibitor binds and inhibits the tyrosine kinase activity of epidermal growth factor receptors, EGFR (or HER1), HER2 and HER4, which leads to reduced phosphorylation and activation of downstream signaling pathways. Neratinib has been shown to be effective against HER2-overexpressing or mutant tumors in vitro and in vivo. Neratinib is currently being investigated in various clinical trials in breast cancers and other solid tumors, including those with HER2 mutation. Earlier studies have already shown promising clinical activity for neratinib. However, more translational research is required to investigate biomarkers that could help to predict response and resistance for selection of appropriate patients for treatment with neratinib, either as monotherapy or in combination with other drug(s). Keywords: neratinib, HKI 272, pan-HER inhibitor, irreversible tyrosine kinase inhibitor, HER (ErbB), breast cancer
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spelling doaj.art-5cb301d1dbae4fba992557e02098628a2022-12-21T22:58:33ZengDove Medical PressBreast Cancer: Targets and Therapy1179-13142015-06-012015default14716222086Profile of neratinib and its potential in the treatment of breast cancerFeldinger KKong AKatharina Feldinger,1 Anthony Kong,2 1Department of Oncology, The Weatherall Institute of Molecular Medicine, University of Oxford, Oxford, 2The Robert Aitkin Institute, School of Cancer Sciences, University of Birmingham, Birmingham, UK Abstract: The HER (ErbB) receptor tyrosine kinase receptors are implicated in many cancers and several anti-HER treatments are now approved. In recent years, a new group of compounds that bind irreversibly to the adenosine triphosphate binding pocket of HER receptors have been developed. One of these compounds, neratinib, has passed preclinical phases and is currently undergoing various clinical trials. This manuscript reviews the preclinical as well as clinical data on neratinib. As a pan-HER inhibitor, this irreversible tyrosine kinase inhibitor binds and inhibits the tyrosine kinase activity of epidermal growth factor receptors, EGFR (or HER1), HER2 and HER4, which leads to reduced phosphorylation and activation of downstream signaling pathways. Neratinib has been shown to be effective against HER2-overexpressing or mutant tumors in vitro and in vivo. Neratinib is currently being investigated in various clinical trials in breast cancers and other solid tumors, including those with HER2 mutation. Earlier studies have already shown promising clinical activity for neratinib. However, more translational research is required to investigate biomarkers that could help to predict response and resistance for selection of appropriate patients for treatment with neratinib, either as monotherapy or in combination with other drug(s). Keywords: neratinib, HKI 272, pan-HER inhibitor, irreversible tyrosine kinase inhibitor, HER (ErbB), breast cancerhttp://www.dovepress.com/profile-of-neratinib-and-its-potential-in-the-treatment-of-breast-canc-peer-reviewed-article-BCTT
spellingShingle Feldinger K
Kong A
Profile of neratinib and its potential in the treatment of breast cancer
Breast Cancer: Targets and Therapy
title Profile of neratinib and its potential in the treatment of breast cancer
title_full Profile of neratinib and its potential in the treatment of breast cancer
title_fullStr Profile of neratinib and its potential in the treatment of breast cancer
title_full_unstemmed Profile of neratinib and its potential in the treatment of breast cancer
title_short Profile of neratinib and its potential in the treatment of breast cancer
title_sort profile of neratinib and its potential in the treatment of breast cancer
url http://www.dovepress.com/profile-of-neratinib-and-its-potential-in-the-treatment-of-breast-canc-peer-reviewed-article-BCTT
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