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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Autores principales:	Feldinger K, Kong A
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2015
Materias:	Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282
Acceso en línea:	https://doaj.org/article/5cb301d1dbae4fba992557e02098628a
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spelling	oai:doaj.org-article:5cb301d1dbae4fba992557e02098628a2021-12-02T07:58:16ZProfile of neratinib and its potential in the treatment of breast cancer1179-1314https://doaj.org/article/5cb301d1dbae4fba992557e02098628a2015-06-01T00:00:00Zhttp://www.dovepress.com/profile-of-neratinib-and-its-potential-in-the-treatment-of-breast-canc-peer-reviewed-article-BCTThttps://doaj.org/toc/1179-1314Katharina 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 cancerFeldinger KKong ADove Medical PressarticleNeoplasms. Tumors. Oncology. Including cancer and carcinogensRC254-282ENBreast Cancer: Targets and Therapy, Vol 2015, Iss default, Pp 147-162 (2015)
institution	DOAJ
collection	DOAJ
language	EN
topic	Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282
spellingShingle	Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282 Feldinger K Kong A Profile of neratinib and its potential in the treatment of breast cancer
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
format	article
author	Feldinger K Kong A
author_facet	Feldinger K Kong A
author_sort	Feldinger K
title	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_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_sort	profile of neratinib and its potential in the treatment of breast cancer
publisher	Dove Medical Press
publishDate	2015
url	https://doaj.org/article/5cb301d1dbae4fba992557e02098628a
work_keys_str_mv	AT feldingerk profileofneratinibanditspotentialinthetreatmentofbreastcancer AT konga profileofneratinibanditspotentialinthetreatmentofbreastcancer
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Profile of neratinib and its potential in the treatment of breast cancer

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