Angiotensin II type 2 receptor signalling as a pain target: Bench, bedside and back-translation

IF 4 3区 医学 Q1 PHARMACOLOGY & PHARMACY
Andrew J. Shepherd , Andrew SC. Rice , Maree T. Smith
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引用次数: 0

Abstract

Translating promising preclinical pain relief data for novel molecules from drug discovery to positive clinical trial outcomes is challenging. The angiotensin II type 2 (AT2) receptor is a clinically-validated target based upon positive proof-of-concept clinical trial data in patients with post-herpetic neuralgia. This trial was conducted because AT2 receptor antagonists evoked pain relief in rodent models of neuropathic pain. EMA401 was selected as the drug candidate based upon its suitable preclinical toxicity and safety profile and good pharmacokinetics. Herein, we provide an overview of the discovery, preclinical and clinical development of EMA401, for the alleviation of peripheral neuropathic pain.

Abstract Image

血管紧张素II型2受体信号作为疼痛靶点:实验、临床和反向翻译
将新分子的临床前疼痛缓解数据从药物发现转化为积极的临床试验结果是具有挑战性的。血管紧张素II 2型(AT2)受体是基于疱疹后神经痛患者积极的概念验证临床试验数据的临床验证靶点。进行这项试验是因为AT2受体拮抗剂在啮齿动物神经性疼痛模型中引起疼痛缓解。EMA401因其适宜的临床前毒性和安全性以及良好的药代动力学而被选为候选药物。在此,我们概述了EMA401的发现,临床前和临床开发,以减轻周围神经性疼痛。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
CiteScore
8.80
自引率
2.50%
发文量
131
审稿时长
4-8 weeks
期刊介绍: Current Opinion in Pharmacology (COPHAR) publishes authoritative, comprehensive, and systematic reviews. COPHAR helps specialists keep up to date with a clear and readable synthesis on current advances in pharmacology and drug discovery. Expert authors annotate the most interesting papers from the expanding volume of information published today, saving valuable time and giving the reader insight on areas of importance.
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