Biodistribution and radiation dosimetry of [68Ga]gallium 2,2'-(7-(4-((1-carboxy-4-((1-((carboxymethyl)amino)-3-((2-((4-(dihydroxyarsaneyl)phenyl)amino)-2-oxoethyl)thio)-1-oxopropan-2-yl)amino)-4-oxobutyl)amino)-1-carboxylato-4-oxobutyl)-1,4,7-triazonane-1,4-diyl)diacetate (68Ga NODAGA GSAO) for positron emission tomography (PET) of cell death in patients with solid malignancies.

This study assesses human biodistribution, radiation dosimetry, safety and tumour uptake of cell death indicator labelled with 68Ga ([68Ga]Ga-CDI), a novel radiopharmaceutical that can image multiple forms of cell death. Five participants with at least one extracranial site of solid malignancy>2 cm and no active cancer treatment in the 8 weeks prior to the study were enrolled. [68Ga] Ga-CDI is safe and well-tolerated with no side effects or adverse events observed. [68Ga]Ga-CDI is renally excreted, demonstrates low levels of physiologic uptake in the other organs and has excellent imaging characteristics. The mean effective dose was 2.17E- 02± 4.61E-03 mSv/MBq. It images constitutive tumour cell death and correlates with tumour cell death on histology. In summary, [68Ga]Ga-CDI is a novel cell death imaging radiopharmaceutical that is safe, has low radiation dosimetry and excellent biodistribution and imaging characteristics. It has potential advantages over previously investigated radiopharmaceuticals for imaging of cell death and has progressed to a proof-of-concept trial.