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A review of the therapeutic role of the new third-generation TKI olverembatinib in chronic myeloid leukemia

Several tyrosine kinase inhibitors (TKIs) have been developed as targeted therapies to inhibit the oncogenic activity of several tyrosine kinases in chronic myeloid leukemia (CML), acute lymphoid leukemia (ALL), gastrointestinal stromal tumor (GIST), and other diseases. TKIs have significantly impro...

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Detalles Bibliográficos
Autores principales: Qian, Honglan, Gang, Dongxu, He, Xiaoyu, Jiang, Songfu
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Frontiers Media S.A. 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9772831/
https://www.ncbi.nlm.nih.gov/pubmed/36568202
http://dx.doi.org/10.3389/fonc.2022.1036437
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author Qian, Honglan
Gang, Dongxu
He, Xiaoyu
Jiang, Songfu
author_facet Qian, Honglan
Gang, Dongxu
He, Xiaoyu
Jiang, Songfu
author_sort Qian, Honglan
collection PubMed
description Several tyrosine kinase inhibitors (TKIs) have been developed as targeted therapies to inhibit the oncogenic activity of several tyrosine kinases in chronic myeloid leukemia (CML), acute lymphoid leukemia (ALL), gastrointestinal stromal tumor (GIST), and other diseases. TKIs have significantly improved the overall survival of these patients and changed the treatment strategy in the clinic. However, approximately 50% of patients develop resistance or intolerance to imatinib. For second-generation TKIs, approximately 30%–40% of patients need to change therapy by 5 years when they are used as first-line treatment. Clinical study analysis showed that the T315I mutation is highly associated with TKI resistance. Developing new drugs that target the T315I mutation will address the dilemma of treatment failure. Olverembatinib, as a third-generation TKI designed for the T315I mutation, is being researched in China. Preliminary clinical data show the safety and efficacy in treating CML patients harboring the T315I mutation or who are resistant to first- or second-line TKI treatment. Herein, we review the characteristics and clinical trials of olverembatinib. We also discuss its role in the management of CML patients.
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spelling pubmed-97728312022-12-23 A review of the therapeutic role of the new third-generation TKI olverembatinib in chronic myeloid leukemia Qian, Honglan Gang, Dongxu He, Xiaoyu Jiang, Songfu Front Oncol Oncology Several tyrosine kinase inhibitors (TKIs) have been developed as targeted therapies to inhibit the oncogenic activity of several tyrosine kinases in chronic myeloid leukemia (CML), acute lymphoid leukemia (ALL), gastrointestinal stromal tumor (GIST), and other diseases. TKIs have significantly improved the overall survival of these patients and changed the treatment strategy in the clinic. However, approximately 50% of patients develop resistance or intolerance to imatinib. For second-generation TKIs, approximately 30%–40% of patients need to change therapy by 5 years when they are used as first-line treatment. Clinical study analysis showed that the T315I mutation is highly associated with TKI resistance. Developing new drugs that target the T315I mutation will address the dilemma of treatment failure. Olverembatinib, as a third-generation TKI designed for the T315I mutation, is being researched in China. Preliminary clinical data show the safety and efficacy in treating CML patients harboring the T315I mutation or who are resistant to first- or second-line TKI treatment. Herein, we review the characteristics and clinical trials of olverembatinib. We also discuss its role in the management of CML patients. Frontiers Media S.A. 2022-12-08 /pmc/articles/PMC9772831/ /pubmed/36568202 http://dx.doi.org/10.3389/fonc.2022.1036437 Text en Copyright © 2022 Qian, Gang, He and Jiang https://creativecommons.org/licenses/by/4.0/This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
spellingShingle Oncology
Qian, Honglan
Gang, Dongxu
He, Xiaoyu
Jiang, Songfu
A review of the therapeutic role of the new third-generation TKI olverembatinib in chronic myeloid leukemia
title A review of the therapeutic role of the new third-generation TKI olverembatinib in chronic myeloid leukemia
title_full A review of the therapeutic role of the new third-generation TKI olverembatinib in chronic myeloid leukemia
title_fullStr A review of the therapeutic role of the new third-generation TKI olverembatinib in chronic myeloid leukemia
title_full_unstemmed A review of the therapeutic role of the new third-generation TKI olverembatinib in chronic myeloid leukemia
title_short A review of the therapeutic role of the new third-generation TKI olverembatinib in chronic myeloid leukemia
title_sort review of the therapeutic role of the new third-generation tki olverembatinib in chronic myeloid leukemia
topic Oncology
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9772831/
https://www.ncbi.nlm.nih.gov/pubmed/36568202
http://dx.doi.org/10.3389/fonc.2022.1036437
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