Preclinical characteristics of the irreversible pan-HER kinase inhibitor neratinib compared with lapatinib : implications for the treatment of HER2-positive and HER2-mutated breast cancer
An estimated 15-20% of breast cancers overexpress human epidermal growth factor receptor 2 (HER2/ERBB2/neu). Two small-molecule tyrosine kinase inhibitors (TKIs), lapatinib and neratinib, have been approved for the treatment of HER2-positive (HER2+) breast cancer. Lapatinib, a reversible epidermal g...
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| Format: | Journal Article |
| Language: | English |
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2020
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| Online Access: | https://hdl.handle.net/10356/142754 |
| _version_ | 1826115177642196992 |
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| author | Collins, Denis M. Conlon, Neil T. Kannan, Srinivasaraghavan Verma, Chandra Shekhar Eli, Lisa D. Lalani, Alshad S. Crown, John |
| author2 | School of Biological Sciences |
| author_facet | School of Biological Sciences Collins, Denis M. Conlon, Neil T. Kannan, Srinivasaraghavan Verma, Chandra Shekhar Eli, Lisa D. Lalani, Alshad S. Crown, John |
| author_sort | Collins, Denis M. |
| collection | NTU |
| description | An estimated 15-20% of breast cancers overexpress human epidermal growth factor receptor 2 (HER2/ERBB2/neu). Two small-molecule tyrosine kinase inhibitors (TKIs), lapatinib and neratinib, have been approved for the treatment of HER2-positive (HER2+) breast cancer. Lapatinib, a reversible epidermal growth factor receptor (EGFR/ERBB1/HER1) and HER2 TKI, is used for the treatment of advanced HER2+ breast cancer in combination with capecitabine, in combination with trastuzumab in patients with hormone receptor-negative metastatic breast cancer, and in combination with an aromatase inhibitor for the first-line treatment of HER2+ breast cancer. Neratinib, a next-generation, irreversible pan-HER TKI, is used in the US for extended adjuvant treatment of adult patients with early-stage HER2+ breast cancer following 1 year of trastuzumab. In Europe, neratinib is used in the extended adjuvant treatment of adult patients with early-stage hormone receptor-positive HER2+ breast cancer who are less than 1 year from the completion of prior adjuvant trastuzumab-based therapy. Preclinical studies have shown that these agents have distinct properties that may impact their clinical activity. This review describes the preclinical characterization of lapatinib and neratinib, with a focus on the differences between these two agents that may have implications for patient management. |
| first_indexed | 2024-10-01T03:50:57Z |
| format | Journal Article |
| id | ntu-10356/142754 |
| institution | Nanyang Technological University |
| language | English |
| last_indexed | 2024-10-01T03:50:57Z |
| publishDate | 2020 |
| record_format | dspace |
| spelling | ntu-10356/1427542023-02-28T17:08:38Z Preclinical characteristics of the irreversible pan-HER kinase inhibitor neratinib compared with lapatinib : implications for the treatment of HER2-positive and HER2-mutated breast cancer Collins, Denis M. Conlon, Neil T. Kannan, Srinivasaraghavan Verma, Chandra Shekhar Eli, Lisa D. Lalani, Alshad S. Crown, John School of Biological Sciences Bioinformatics Institute, A*STAR Science::Biological sciences Tyrosine Kinase Inhibitors Lapatinib An estimated 15-20% of breast cancers overexpress human epidermal growth factor receptor 2 (HER2/ERBB2/neu). Two small-molecule tyrosine kinase inhibitors (TKIs), lapatinib and neratinib, have been approved for the treatment of HER2-positive (HER2+) breast cancer. Lapatinib, a reversible epidermal growth factor receptor (EGFR/ERBB1/HER1) and HER2 TKI, is used for the treatment of advanced HER2+ breast cancer in combination with capecitabine, in combination with trastuzumab in patients with hormone receptor-negative metastatic breast cancer, and in combination with an aromatase inhibitor for the first-line treatment of HER2+ breast cancer. Neratinib, a next-generation, irreversible pan-HER TKI, is used in the US for extended adjuvant treatment of adult patients with early-stage HER2+ breast cancer following 1 year of trastuzumab. In Europe, neratinib is used in the extended adjuvant treatment of adult patients with early-stage hormone receptor-positive HER2+ breast cancer who are less than 1 year from the completion of prior adjuvant trastuzumab-based therapy. Preclinical studies have shown that these agents have distinct properties that may impact their clinical activity. This review describes the preclinical characterization of lapatinib and neratinib, with a focus on the differences between these two agents that may have implications for patient management. Published version 2020-06-30T00:57:53Z 2020-06-30T00:57:53Z 2019 Journal Article Collins, D. M., Conlon, N. T., Kannan, S., Verma, C. S., Eli, L. D., Lalani, A. S., & Crown, J. (2019). Preclinical characteristics of the irreversible pan-HER kinase inhibitor neratinib compared with lapatinib : implications for the treatment of HER2-positive and HER2-mutated breast cancer. Cancers, 11(6), 737-. doi:10.3390/cancers11060737 2072-6694 https://hdl.handle.net/10356/142754 10.3390/cancers11060737 31141894 2-s2.0-85069437053 6 11 en Cancers © 2019 The Authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). application/pdf |
| spellingShingle | Science::Biological sciences Tyrosine Kinase Inhibitors Lapatinib Collins, Denis M. Conlon, Neil T. Kannan, Srinivasaraghavan Verma, Chandra Shekhar Eli, Lisa D. Lalani, Alshad S. Crown, John Preclinical characteristics of the irreversible pan-HER kinase inhibitor neratinib compared with lapatinib : implications for the treatment of HER2-positive and HER2-mutated breast cancer |
| title | Preclinical characteristics of the irreversible pan-HER kinase inhibitor neratinib compared with lapatinib : implications for the treatment of HER2-positive and HER2-mutated breast cancer |
| title_full | Preclinical characteristics of the irreversible pan-HER kinase inhibitor neratinib compared with lapatinib : implications for the treatment of HER2-positive and HER2-mutated breast cancer |
| title_fullStr | Preclinical characteristics of the irreversible pan-HER kinase inhibitor neratinib compared with lapatinib : implications for the treatment of HER2-positive and HER2-mutated breast cancer |
| title_full_unstemmed | Preclinical characteristics of the irreversible pan-HER kinase inhibitor neratinib compared with lapatinib : implications for the treatment of HER2-positive and HER2-mutated breast cancer |
| title_short | Preclinical characteristics of the irreversible pan-HER kinase inhibitor neratinib compared with lapatinib : implications for the treatment of HER2-positive and HER2-mutated breast cancer |
| title_sort | preclinical characteristics of the irreversible pan her kinase inhibitor neratinib compared with lapatinib implications for the treatment of her2 positive and her2 mutated breast cancer |
| topic | Science::Biological sciences Tyrosine Kinase Inhibitors Lapatinib |
| url | https://hdl.handle.net/10356/142754 |
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