αvβ6和αvβ1整合素抑制治疗特发性肺纤维化的潜力。

IF 4.6 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Expert Opinion on Therapeutic Targets Pub Date : 2024-07-01 Epub Date: 2024-07-02 DOI:10.1080/14728222.2024.2375375
Serena Bellani, Philip L Molyneaux, Toby M Maher, Paolo Spagnolo
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引用次数: 0

摘要

简介特发性肺纤维化(IPF)是一种慢性进展性间质性肺病,病因不明,预后不良。全球已批准使用 Nintedanib 和 Pirfenidone 治疗 IPF,但这两种药物只能减缓功能衰退和疾病进展的速度。αvβ6和αvβ1是纤维化组织中过度表达的两种整合素,在肺纤维化的发展过程中起着至关重要的作用。它们通过将转化生长因子(TGF)-β(最重要的促纤维化细胞因子之一)转化为活性形式而发挥作用。在此,我们对αvβ6/αvβ1整合素双重抑制剂治疗IPF的潜力进行了总结和批判性讨论:Bexotegrast是一种双重αvβ6/αvβ1整合素抑制剂,具有减缓甚至阻止IPF疾病进展的潜力。事实上,强大的临床前理论依据和充满希望的早期临床试验数据让人们对其充满了期待。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Potential of αvβ6 and αvβ1 integrin inhibition for treatment of idiopathic pulmonary fibrosis.

Introduction: Idiopathic pulmonary fibrosis (IPF) is a chronic progressive interstitial lung disease of unknown cause with a dismal prognosis. Nintedanib and Pirfenidone are approved worldwide for the treatment of IPF, but they only slow the rate of functional decline and disease progression. Therefore, there is an urgent need for more efficacious and better tolerated drugs.

Areas covered: αvβ6 and αvβ1 are two integrins overexpressed in fibrotic tissue, which play a critical role in the development of lung fibrosis. They act by converting transforming growth factor (TGF)-β, one of the most important profibrotic cytokine, in its active form. Here, we summarize and critically discuss the potential of a dual αvβ6/αvβ1 integrin inhibitor for the treatment of IPF.

Expert opinion: Bexotegrast, a dual αvβ6/αvβ1 integrin inhibitor, has the potential to slow or even halt disease progression in IPF. Indeed, the strong pre-clinical rationale and promising early phase clinical trial data have raised expectations.

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来源期刊
CiteScore
8.90
自引率
1.70%
发文量
58
审稿时长
3 months
期刊介绍: The journal evaluates molecules, signalling pathways, receptors and other therapeutic targets and their potential as candidates for drug development. Articles in this journal focus on the molecular level and early preclinical studies. Articles should not include clinical information including specific drugs and clinical trials. The Editors welcome: Reviews covering novel disease targets at the molecular level and information on early preclinical studies and their implications for future drug development. Articles should not include clinical information including specific drugs and clinical trials. Original research papers reporting results of target selection and validation studies and basic mechanism of action studies for investigative and marketed drugs. The audience consists of scientists, managers and decision makers in the pharmaceutical industry, academic researchers working in the field of molecular medicine and others closely involved in R&D.
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