Skip to main content

REVIEW article

Front. Pharmacol.
Sec. Pharmacology of Anti-Cancer Drugs
Volume 15 - 2024 | doi: 10.3389/fphar.2024.1463520
This article is part of the Research Topic Innovative Approaches to Overcome Resistance and Toxicities of Anti-Cancer Drugs View all 21 articles

Endothelin receptor antagonists (ERAs) can potentially be used as therapeutic drugs to reduce hypertension caused by small molecule tyrosine kinase inhibitors (TKIs)

Provisionally accepted
Qingjian He Qingjian He 1Junling Lin Junling Lin 1Chanjuan Mo Chanjuan Mo 1Guodong Li Guodong Li 1Jianzhong Lu Jianzhong Lu 1Qiyin Sun Qiyin Sun 1Lijun Cao Lijun Cao 1Haojian Gan Haojian Gan 2Quan Sun Quan Sun 2Jiafang Yao Jiafang Yao 1Shengyi Lian Shengyi Lian 1Wenjuan Wang Wenjuan Wang 1*
  • 1 The First People's Hospital of Huzhou, Huzhou, China
  • 2 Schools of Medicine and Nursing Sciences, Huzhou University, Huzhou, China

The final, formatted version of the article will be published soon.

    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.

    Keywords: Hypertension, tyrosine kinase inhibitors, Endothelin receptor antagonists, endothelin, aprocitentan

    Received: 12 Jul 2024; Accepted: 23 Dec 2024.

    Copyright: © 2024 He, Lin, Mo, Li, Lu, Sun, Cao, Gan, Sun, Yao, Lian and Wang. 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) or licensor 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.

    * Correspondence: Wenjuan Wang, The First People's Hospital of Huzhou, Huzhou, China

    Disclaimer: All claims expressed in this article are solely those of the authors and do not necessarily represent those of their affiliated organizations, or those of the publisher, the editors and the reviewers. Any product that may be evaluated in this article or claim that may be made by its manufacturer is not guaranteed or endorsed by the publisher.