Positron emission tomography (PET) is an extensively used nuclear functional imaging technique, especially for central nervous system (CNS) and oncological disorders. Currently, drug development is a lengthy and costly pursuit. Imaging with PET radiotracers could be an effective way to hasten drug discovery and advancement, because it facilitates the monitoring of key facets, such as receptor occupancy quantification, drug biodistribution, pharmacokinetic (PK) analyses, validation of target engagement, treatment monitoring, and measurement of neurotransmitter concentrations. These parameters demand careful analyses for the robust appraisal of newly formulated drugs during preclinical and clinical trials. In this review, we discuss the usage of PET imaging in radiopharmaceutical development; drug development approaches with PET imaging; and PET developments in oncological and cardiac drug discovery.

正电子发射断层扫描 (PET) 是一种广泛使用的核功能成像技术，尤其适用于中枢神经系统 (CNS) 和肿瘤疾病。目前，药物开发是一项漫长而昂贵的追求。使用 PET 放射性示踪剂成像可能是加速药物发现和进步的有效方法，因为它有助于监测关键方面，例如受体占据量化、药物生物分布、药代动力学 (PK) 分析、靶标参与验证、治疗监测和测量的神经递质浓度。这些参数需要仔细分析，以便在临床前和临床试验期间对新配方药物进行强有力的评估。在这篇综述中，我们讨论了 PET 成像在放射性药物开发中的应用；PET成像的药物开发方法；