Endothelin receptor antagonists (ERAs) can potentially be used as therapeutic drugs to reduce hypertension caused by small molecule tyrosine kinase inhibitors (TKIs)
The emergence of targeted anti-tumor drugs has significantly prolonged the lifespan and improved the prognosis of cancer patients. Among these drugs, vascular endothelial growth factor (VEGF) inhibitors, particularly novel small molecule tyrosine kinase inhibitors (TKIs), are extensively employed as...
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Frontiers Media S.A.
2025-01-01
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Series: | Frontiers in Pharmacology |
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Online Access: | https://www.frontiersin.org/articles/10.3389/fphar.2024.1463520/full |
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author | Qingjian He Junling Lin Chanjuan Mo Guodong Li Jianzhong Lu Qiyin Sun Lijun Cao Haojian Gan Quan Sun Jiafang Yao Shengyi Lian WenJuan Wang |
author_facet | Qingjian He Junling Lin Chanjuan Mo Guodong Li Jianzhong Lu Qiyin Sun Lijun Cao Haojian Gan Quan Sun Jiafang Yao Shengyi Lian WenJuan Wang |
author_sort | Qingjian He |
collection | DOAJ |
description | The emergence of targeted anti-tumor drugs has significantly prolonged the lifespan and improved the prognosis of cancer patients. Among these drugs, vascular endothelial growth factor (VEGF) inhibitors, particularly novel small molecule tyrosine kinase inhibitors (TKIs), are extensively employed as VEGF inhibitors; however, they are also associated with a higher incidence of complications, with hypertension being the most prevalent cardiovascular toxic side effect. Currently, it is widely accepted that TKIs-induced hypertension involves multiple mechanisms including dysregulation of the endothelin (ET) axis, reduced bioavailability of nitric oxide (NO), imbalance in NO-ROS equilibrium system, vascular rarefaction, and activation of epithelial sodium calcium channels; nevertheless, excessive activation of ET system appears to be predominantly responsible for this condition. Moreover, studies have demonstrated that ET plays a pivotal role in driving TKIs-induced hypertension. Therefore, this review aims to explore the significance of ET in the pathogenesis of hypertension induced by targeted anti-tumor drugs and investigate the potential therapeutic value of endothelin antagonists in managing hypertension caused by targeted anti-tumor drugs. |
format | Article |
id | doaj-art-69f1c5e071704ebb8c22e4314dbfe095 |
institution | Kabale University |
issn | 1663-9812 |
language | English |
publishDate | 2025-01-01 |
publisher | Frontiers Media S.A. |
record_format | Article |
series | Frontiers in Pharmacology |
spelling | doaj-art-69f1c5e071704ebb8c22e4314dbfe0952025-01-09T06:10:12ZengFrontiers Media S.A.Frontiers in Pharmacology1663-98122025-01-011510.3389/fphar.2024.14635201463520Endothelin receptor antagonists (ERAs) can potentially be used as therapeutic drugs to reduce hypertension caused by small molecule tyrosine kinase inhibitors (TKIs)Qingjian He0Junling Lin1Chanjuan Mo2Guodong Li3Jianzhong Lu4Qiyin Sun5Lijun Cao6Haojian Gan7Quan Sun8Jiafang Yao9Shengyi Lian10WenJuan Wang11Department of Breast and Thyroid Surgery, First Affiliated Hospital of Huzhou University, Huzhou, ChinaDepartment of Cardiovascular Center, First Affiliated Hospital of Huzhou University, Huzhou, ChinaDepartment of Cardiovascular Center, First Affiliated Hospital of Huzhou University, Huzhou, ChinaDepartment of Cardiovascular Center, First Affiliated Hospital of Huzhou University, Huzhou, ChinaDepartment of Cardiovascular Center, First Affiliated Hospital of Huzhou University, Huzhou, ChinaDepartment of Cardiovascular Center, First Affiliated Hospital of Huzhou University, Huzhou, ChinaDepartment of Cardiovascular Center, First Affiliated Hospital of Huzhou University, Huzhou, ChinaSchool of Medicine, Huzhou University, Huzhou, ChinaSchool of Medicine, Huzhou University, Huzhou, ChinaDepartment of Cardiovascular Center, First Affiliated Hospital of Huzhou University, Huzhou, ChinaDepartment of Cardiovascular Center, First Affiliated Hospital of Huzhou University, Huzhou, ChinaDepartment of Cardiovascular Center, First Affiliated Hospital of Huzhou University, Huzhou, ChinaThe emergence of targeted anti-tumor drugs has significantly prolonged the lifespan and improved the prognosis of cancer patients. Among these drugs, vascular endothelial growth factor (VEGF) inhibitors, particularly novel small molecule tyrosine kinase inhibitors (TKIs), are extensively employed as VEGF inhibitors; however, they are also associated with a higher incidence of complications, with hypertension being the most prevalent cardiovascular toxic side effect. Currently, it is widely accepted that TKIs-induced hypertension involves multiple mechanisms including dysregulation of the endothelin (ET) axis, reduced bioavailability of nitric oxide (NO), imbalance in NO-ROS equilibrium system, vascular rarefaction, and activation of epithelial sodium calcium channels; nevertheless, excessive activation of ET system appears to be predominantly responsible for this condition. Moreover, studies have demonstrated that ET plays a pivotal role in driving TKIs-induced hypertension. Therefore, this review aims to explore the significance of ET in the pathogenesis of hypertension induced by targeted anti-tumor drugs and investigate the potential therapeutic value of endothelin antagonists in managing hypertension caused by targeted anti-tumor drugs.https://www.frontiersin.org/articles/10.3389/fphar.2024.1463520/fullhypertensiontyrosine kinase inhibitorsendothelin receptor antagonistsendothelinaprocitentan |
spellingShingle | Qingjian He Junling Lin Chanjuan Mo Guodong Li Jianzhong Lu Qiyin Sun Lijun Cao Haojian Gan Quan Sun Jiafang Yao Shengyi Lian WenJuan Wang Endothelin receptor antagonists (ERAs) can potentially be used as therapeutic drugs to reduce hypertension caused by small molecule tyrosine kinase inhibitors (TKIs) Frontiers in Pharmacology hypertension tyrosine kinase inhibitors endothelin receptor antagonists endothelin aprocitentan |
title | Endothelin receptor antagonists (ERAs) can potentially be used as therapeutic drugs to reduce hypertension caused by small molecule tyrosine kinase inhibitors (TKIs) |
title_full | Endothelin receptor antagonists (ERAs) can potentially be used as therapeutic drugs to reduce hypertension caused by small molecule tyrosine kinase inhibitors (TKIs) |
title_fullStr | Endothelin receptor antagonists (ERAs) can potentially be used as therapeutic drugs to reduce hypertension caused by small molecule tyrosine kinase inhibitors (TKIs) |
title_full_unstemmed | Endothelin receptor antagonists (ERAs) can potentially be used as therapeutic drugs to reduce hypertension caused by small molecule tyrosine kinase inhibitors (TKIs) |
title_short | Endothelin receptor antagonists (ERAs) can potentially be used as therapeutic drugs to reduce hypertension caused by small molecule tyrosine kinase inhibitors (TKIs) |
title_sort | endothelin receptor antagonists eras can potentially be used as therapeutic drugs to reduce hypertension caused by small molecule tyrosine kinase inhibitors tkis |
topic | hypertension tyrosine kinase inhibitors endothelin receptor antagonists endothelin aprocitentan |
url | https://www.frontiersin.org/articles/10.3389/fphar.2024.1463520/full |
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