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Gallium-67/Gallium-68-[DFO]-Octreotide—A Potential Radiopharmaceutical for PET Imaging of Somatostatin Receptor-Positive Tumors: Synthesis and Radiolabeling In Vitro and Preliminary In Vivo Studies

Institute of Nuclear Medicine, University Hospital
Preclinical Research, Sandoz Limited, Basel
Paul Scherrer Institute, Villigen, Switzerland

Correspondence: For correspondence or reprints contact: P.M. Smith-Jones, Building 386 Lab. 622, Preclinical Research, c/o Sandoz Pharma, CH 4002 Basel, Switzerland.

ABSTRACT

When labeled with gamma-emitting radionuclides, somatostatin analogs have the potential to localize somatostatin receptor-positive tumors using gamma camera scintigtaphy. We present a somatostatin analog, [DFO]-octreotide (SDZ 216-927), that comprises desferrioxamine B coupled to octreotide via succinyl linker. This conjugate can be labeled with either ⁶⁷Ga for gamma scintigraphy or ⁶⁸Ga for PET imaging. The ⁶⁷Ga-labaled conjugate is stable in vitro to autoradiolysis over a 24-hr period. Methods: Rats bearing a somatostatin receptor-positive pancreatic islet cell tumor were injected with 20 MBq of ⁶⁷Ga[DFO]-octreotide (33 GBq ⁶⁷Ga/µmole). Results: After 1 hr. the accumulation of ⁶⁷Ga[DFO]-octreotide was 0.38 ± 0.08 %ID/g and the tumor-to-nontumor ratios for blood, muscle, liver and intestine were 2.5, 7.4, 1.9 and 1.6, respectively. PET studies with ⁶⁸Ga[DFO]-octreotide recorded a very rapid accumulation at the tumor and a subsequent residence half-life of about 6 hr. Conclusion: Gallium-68-[DFO]-octreotide can be used in PET studies to diagnose receptor-positive tumors such as gastroentero-pancreatic, small-cell lung and breast tumors.

Key Words: somatostatin receptors • octreotide • gallium-68 • gallium-67

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