Gallium-68 Labelled Radiopharmaceuticals for Imaging Inflammatory Disorders

Inflammation is an important component of several chronic and debilitating diseases that result in significant morbidity and mortality. This is best evidenced within the cardiovascular system where it may manifest as atherosclerosis or myocarditis, and at the extreme end of the spectrum as myocardial infarction, ventricular remodeling, or cardiac failure. Early non-invasive detection and monitoring of inflammation in these and other settings may better guide patient management with resultant improved outcomes.Key role players in inflammation pathophysiology include chemokines, macrophages, neu-trophils, fibroblasts, integrins, and reactive oxygen species, amongst others. Examples of receptor expression and over-expression include somatostatin receptors, CXCR4-, folate-, mannose-, TSPO-receptors and secretion of various vascular adhesion molecules (such as VCAM and ICAM).Gallium-68-based PET offers imaging possibilities for nearly all the major pathophysiologi-cal role players in inflammation, with mounting recent interest in macrophage differentia-tion, various forms of receptor expression and secretion of chemokines and vascular adhesion molecules. The advantages in terms of logistics and costs of having generator -produced PET probes available is well known, and a 68Ga-based tracer provides easily translatable theranostic possibilities to especially Lu-177.Some of the more versatile and better validated Ga-68-based inflammation probes include 68Ga-DOTA-TATE/NOC/TOC, 68Ga-NOTA-RGD, 68Ga-CXCR4, 68Ga-citrate and 68Ga-FAPI. Semin Nucl Med 53:199-212 (c) 2022 Elsevier Inc. All rights reserved.

Automated summary

Inflammation plays a crucial role in various chronic diseases, especially within the cardiovascular system. Early detection and monitoring of inflammation can improve patient management and outcomes. Key factors involved in inflammation pathophysiology include chemokines, macrophages, neutrophils, fibroblasts, integrins, and reactive oxygen species.