Approaching Gallium-68 radiopharmaceuticals for tumor diagnosis: a Medicinal Chemist's perspective

IF 6 2区医学 Q1 CHEMISTRY, MEDICINAL

European Journal of Medicinal Chemistry Pub Date : 2025-05-14 DOI:10.1016/j.ejmech.2025.117760

Francesca Musumeci , Alessandro Fasce , Marta Falesiedi, Federica Oleari, Giancarlo Grossi, Anna Carbone, Silvia Schenone

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引用次数: 0

Abstract

Nuclear medicine has revolutionized disease diagnosis and treatment, particularly in oncology, by enabling precise imaging and targeted therapies using radiopharmaceuticals. Recently, Gallium-68 (⁶⁸Ga) has emerged as a powerful positron emission tomography (PET) imaging agent, with a growing role in theranostics when paired with ¹⁷⁷Lu for cancer treatment. The ability to obtain ⁶⁸Ga from ⁶⁸Ge/⁶⁸Ga generators, along with its favorable radiochemical and pharmacokinetic properties, has driven an increasing number of clinical applications, which culminated with the approvals of ⁶⁸Ga-DOTA-TOC and ⁶⁸Ga-DOTA-TATE for the treatment of neuroendocrine tumors, and ⁶⁸Ga-PSMA-11 for prostate cancer over the past decade. This review provides a comprehensive overview of ⁶⁸Ga radiochemistry, chelators, and key compounds in clinical trials, highlighting the potential of this radionuclide in precision oncology.

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接近镓-68放射性药物用于肿瘤诊断：一个药物化学家的观点

核医学通过使用放射性药物实现精确成像和靶向治疗，彻底改变了疾病的诊断和治疗，特别是在肿瘤学方面。最近，镓-68 （68Ga）作为一种强大的正电子发射断层扫描（PET）显像剂出现，当与177Lu配对用于癌症治疗时，在治疗学中的作用越来越大。从68Ge/68Ga发生器中获得68Ga的能力，以及其良好的放射化学和药代动力学特性，推动了越来越多的临床应用，在过去的十年中，68Ga- dota - toc和68Ga- dota - tate被批准用于治疗神经内分泌肿瘤，68Ga- psma -11被批准用于治疗前列腺癌。本文综述了68Ga放射化学、螯合剂和临床试验中的关键化合物，强调了该放射性核素在精确肿瘤学中的潜力。

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来源期刊

European Journal of Medicinal Chemistry 化学-医药化学

CiteScore

11.70

自引率

9.00%

发文量

863

审稿时长

29 days

期刊介绍： The European Journal of Medicinal Chemistry is a global journal that publishes studies on all aspects of medicinal chemistry. It provides a medium for publication of original papers and also welcomes critical review papers. A typical paper would report on the organic synthesis, characterization and pharmacological evaluation of compounds. Other topics of interest are drug design, QSAR, molecular modeling, drug-receptor interactions, molecular aspects of drug metabolism, prodrug synthesis and drug targeting. The journal expects manuscripts to present the rational for a study, provide insight into the design of compounds or understanding of mechanism, or clarify the targets.