正电子发射断层成像(PET)在精神药物发现中的最新应用。

IF 6 2区 医学 Q1 PHARMACOLOGY & PHARMACY Expert Opinion on Drug Discovery Pub Date : 2024-02-01 DOI:10.1080/17460441.2023.2278635
Luc Zimmer
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引用次数: 0

摘要

引言:精神病学是治疗手段缺乏创新的医学学科之一。候选药物试验中的许多失败可以用上游在脑通道、脑靶点结合和临床结果方面评估不佳的药理学特性来解释。正电子发射断层扫描可以提供药代动力学和药效学数据,帮助选择候选分子进行进一步的临床试验。涵盖领域:本综述旨在解释和讨论使用正电子发射放射性标记分子来追踪候选药物的大脑分布或间接测量其与治疗靶点的结合的各种方法。这篇文章不仅仅是对精神药理学PET研究的详尽综述,还强调了这项技术在应用于精神病学的药物发现方面的贡献。专家意见:PET神经成像是唯一一种可以在人体内测量候选药物的大脑输送、靶点结合的百分比和持续时间,甚至药理学效果的技术方法。因此,在精神药物开发的早期阶段对少数受试者进行的PET研究可以提供后续临床评估所需的药代动力学/药效学数据。虽然PET技术在放射化学、放射药理学和核医学专业知识方面要求很高,但它与精神病学新药开发过程的结合具有很大的附加值。
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Recent applications of positron emission tomographic (PET) imaging in psychiatric drug discovery.

Introduction: Psychiatry is one of the medical disciplines that suffers most from a lack of innovation in its therapeutic arsenal. Many failures in drug candidate trials can be explained by pharmacological properties that have been poorly assessed upstream, in terms of brain passage, brain target binding and clinical outcomes. Positron emission tomography can provide pharmacokinetic and pharmacodynamic data to help select candidate-molecules for further clinical trials.

Areas covered: This review aims to explain and discuss the various methods using positron-emitting radiolabeled molecules to trace the cerebral distribution of the drug-candidate or indirectly measure binding to its therapeutic target. More than an exhaustive review of PET studies in psychopharmacology, this article highlights the contributions this technology can make in drug discovery applied to psychiatry.

Expert opinion: PET neuroimaging is the only technological approach that can, in vivo in humans, measure cerebral delivery of a drug candidate, percentage and duration of target binding, and even the pharmacological effects. PET studies in a small number of subjects in the early stages of the development of a psychotropic drug can therefore provide the pharmacokinetic/pharmacodynamic data required for subsequent clinical evaluation. While PET technology is demanding in terms of radiochemical, radiopharmacological and nuclear medicine expertise, its integration into the development process of new drugs for psychiatry has great added value.

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来源期刊
CiteScore
10.20
自引率
1.60%
发文量
78
审稿时长
6-12 weeks
期刊介绍: Expert Opinion on Drug Discovery (ISSN 1746-0441 [print], 1746-045X [electronic]) is a MEDLINE-indexed, peer-reviewed, international journal publishing review articles on novel technologies involved in the drug discovery process, leading to new leads and reduced attrition rates. Each article is structured to incorporate the author’s own expert opinion on the scope for future development. The Editors welcome: Reviews covering chemoinformatics; bioinformatics; assay development; novel screening technologies; in vitro/in vivo models; structure-based drug design; systems biology Drug Case Histories examining the steps involved in the preclinical and clinical development of a particular drug The audience consists of scientists and managers in the healthcare and pharmaceutical industry, academic pharmaceutical scientists and other closely related professionals looking to enhance the success of their drug candidates through optimisation at the preclinical level.
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