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, neutrophils, 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 pathophysiological role players in inflammation, with mounting recent interest in macrophage differentiation, 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.