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肿瘤血管生成靶向酪氨酸激酶抑制剂治疗领域中心脏肿瘤学的进展与展望

Conquests and perspectives of cardio-oncology in the field of tumor angiogenesis-targeting tyrosine kinase inhibitor-based therapy.

作者信息

Bronte Giuseppe, Bronte Enrico, Novo Giuseppina, Pernice Gianfranco, Lo Vullo Francesca, Musso Emmanuela, Bronte Fabrizio, Gulotta Eliana, Rizzo Sergio, Rolfo Christian, Silvestris Nicola, Bazan Viviana, Novo Salvatore, Russo Antonio

机构信息

University of Palermo, Department of Surgical, Oncological and Oral Sciences , Palermo , Italy.

出版信息

Expert Opin Drug Saf. 2015 Feb;14(2):253-67. doi: 10.1517/14740338.2015.986092. Epub 2014 Dec 13.

DOI:10.1517/14740338.2015.986092
PMID:25494575
Abstract

INTRODUCTION

Angiogenesis is fundamental for tumor development and progression. Hence, anti-angiogenic drugs have been developed to target VEGF and its receptors (VEGFRs). Several tyrosine kinase inhibitors (TKIs) have been developed over the years and others are still under investigation, each anti-VEGFR TKI showing a different cardiotoxic profile. Knowledge of the cardiac side-effects of each drug and the magnitude of their expression and frequency can lead to a specific approach.

AREAS COVERED

This work reviews the mechanism of action of anti-VEGFR TKIs and the pathophysiological mechanisms leading to cardiotoxicity, followed by close examination of the most important drugs individually. A literature search was conducted on PubMed selecting review articles, original studies and clinical trials, with a focus on Phase III studies.

EXPERT OPINION

Side-effects on the cardiovascular system could lead both to the worsening of general health status of cancer patients and to the discontinuation of the cancer treatment affecting its efficacy. Cardiologists often have to face new triggers of heart disease in these patients. They need a specific approach, which must be carried out in cooperation with oncologists. It must start before cancer treatment, continue during it and extend after its completion.

摘要

引言

血管生成是肿瘤发生和发展的基础。因此,已开发出抗血管生成药物来靶向血管内皮生长因子(VEGF)及其受体(VEGFRs)。多年来已开发出几种酪氨酸激酶抑制剂(TKIs),其他药物仍在研究中,每种抗VEGFR TKI都表现出不同的心脏毒性特征。了解每种药物的心脏副作用及其表达程度和频率,可采取针对性方法。

涵盖领域

本文综述了抗VEGFR TKIs的作用机制以及导致心脏毒性的病理生理机制,随后对最重要的药物逐一进行详细分析。在PubMed上进行了文献检索,选择综述文章、原创研究和临床试验,重点关注III期研究。

专家观点

心血管系统的副作用可能导致癌症患者总体健康状况恶化,以及影响癌症治疗疗效而导致治疗中断。心脏病专家在这些患者中常常不得不面对新的心脏病诱因。他们需要一种特定的方法,且必须与肿瘤学家合作实施。该方法必须在癌症治疗前开始,治疗期间持续进行,并在治疗结束后继续。

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