In vitro and in vivo studies of three radiolabelled somatostatin analogues:123I-Octreotide (OCT),123I-Tyr-3-OCT and111In-TIRA-d-Phe-1-OCT

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Abstract
Scintigraphy with long-acting somatostatin (SST) analogues may be useful for the localization of tumours expressing receptors (R) for SST. In this study we have analysed the in vitro and in vivo binding properties of three SST analogues,123I-octreotide (OCT),123I-Tyr-3-OCT and111In-DTPA-d-Phe-l-OCT. In vitro binding studies performed with a variety of primary tumours (n=48) as well as with several tumour cell lines (A431, HT29, PANC1, COLO320, HMC1, KU812) indicated significant in vitro binding of these three radiolabelled SST analogues to two subpopulations of SSTR, high (K d 0.2–2.0 nM) and low (K d 5–15 nM) affinity ones. The number of SSTR on tumour cells was at least a 1000-fold higher as compared with normal peripheral blood cells. Comparative scintigraphic studies using123I-OCT and/or123I-Tyr-3-OCT and/or111In-DTPA-d-Phe-1-OCT were performed in 21 patients with histologically verified intestinal carcinoid tumours. Corresponding scintigraphic results were obtained in 18 of 21 patients investigated with two different SSTR ligands, either123I-OCT/123I-Tyr-3-OCT (four of five),123I-OCT/111In-DTPA-d-Phe-1-OCT (eight of nine), or123I-Tyr-3-OCT/111In-DTPA-d-Phe-1-OCT (six of seven). We conclude that various tumours express high amounts of SSTR which are recognized by three radiolabelled SST analogues:123I-OCT,123I-Tyr-3-OCT and111In-DTPA-d-Phe-1-OCT. Differences between these SST analogues in their in vitro binding and/or in vivo scanning properties are observed in a minority of patients. Thus, the labelling of OCT with iodine may be an alternative approach for those nuclear medicine departments for which111In-DTPA-d-Phe-1-OCT is not easily available, or is too expensive.