PET imaging of microglia by targeting macrophage colony-stimulating factor 1 receptor (CSF1R)

Significance[11C]CPPC [5-cyano-N-(4-(4-[11C]methylpiperazin-1-yl)-2-(piperidin-1-yl)phenyl)furan-2-carboxamide] is a PET radiotracer specific for CSF1R, a microglia-specific marker. This compound can be used as a noninvasive tool for imaging of reactive microglia, disease-associated microglia and their contribution to neuroinflammation in vivo. Neuroinflammation is posited to be an underlying pathogenic feature of a wide variety of neuropsychiatric disorders. [11C]CPPC may also be used to study specifically the immune environment of malignancies of the central nervous system and to monitor potential adverse neuroinflammatory effects of immunotherapy for peripheral malignancies. This PET agent will be valuable in the development of new therapeutics for neuroinflammation, particularly those targeting CSF1R, not only by providing a noninvasive, repeatable readout in patients but also by enabling measurement of drug target engagement.

PET imaging of microglia by targeting macrophage colony-stimulating factor 1 receptor (CSF1R) Journal Articles