[Ga-68]Ga-DATATOC imaging, biodistribution and kinetics in a pheochromocytoma model

Objectives The novel DATA (6-Amino-1,4-diazepine-triacetate) based octreotide derivative TOC allows radiolabeling at room temperature in contrast to DOTATOC that needs 95°C for effective labeling. The main goal of this study was to evaluate the potential of [⁶⁸Ga]Ga-DATATOC for SSTR2 imaging in a syngeneic mouse pheochromocytoma (Pheo) model.

Methods Radiolabeling of the DATATOC with ⁶⁸Ga was performed manually at room temperature. The in vivo studies (PET, metabolic stability, biodistribution and elimination) were carried out in Pheo (MPC-mCherry) bearing mice and Wistar rats. For comparison the pheo were also imaged with [⁶⁸Ga]Ga-DOTATOC and [⁶⁸Ga]Ga-DOTATATE. Blocking studies in vivo were performed with octreotide (OC).

Results The radiotracer showed high in vivo stability. A faster renal elimination of the radiotracer was observed in comparison to DOTATOC and DOTATATE. [⁶⁸Ga]Ga-DATATOC showed fast, highly specific uptake in the pheo and the pancreas (SUV at 1 h p.i., tumor 3.7 ± 1.5, pancreas 0.57 ± 0.17), whereas blocking with OC (3.3 mg/kg body weight) reduced the uptake in the tumor to 0.45 ± 0.15 and Patlak analysis showed that both parameters - the influx rate and the distribution volume - were significantly decreased by OC.

Conclusions [⁶⁸Ga]Ga-DATATOC can be radiolabeled with ⁶⁸Ga rapidly at room temperature with high radiochemical yields. The preclinical in vivo studies confirm the high stability, excellent specific targeting and fast elimination. This pharmacological profile and the perspective towards a kit-type formulation provide a great potential for diagnostic somatostatin receptor imaging.

Research Support This work was supported by The Deutsche Forschungsgemeinschaft (Grants ZI-1362/2-1 [to C.G.Z. and G.E.] and BE-2607/1-1 [to R.B. and J.P.]).