Radioiodinated meta-iodobenzylguanidine (MIBG) is used routinely for imaging and targeted radiotherapy of tumours derived from the neural crest. Since active uptake of MIBG by the noradrenaline transporter (NAT) makes a greater contribution to total drug accumulation than passive uptake when MIBG is present at low concentrations, tumour-specific uptake should be enhanced by the administration of lower molar amounts of MIBG. This could be achieved through the use of MIBG with a high specific activity. Commercially available preparations of 123I-MIBG have specific activities of approximately 200 MBq.mg-1. We have synthesized and used no-carrier-added (n.c.a.) 123I-MIBG produced by an iododesilylation reaction (specific activity 0.7 TBq.mg-1). We report here the first clinical studies comparing the commercially available and n.c.a. MIBG diagnostic preparations. Five patients with known phaeochromocytoma were studied. Unlike studies in animal models, no consistent improvement in tumour uptake was observed with the n.c.a. material. A larger patient group is required to determine whether there are significant differences between the two preparations, before proceeding to studies at therapeutic activity levels of n.c.a. 131I-MIBG. Even with no improvement in tumour uptake, n.c.a. MIBG may be the favoured formulation for therapeutic applications to reduce the molar amount of drug injected.

No abstract

Technetium-99m (99Tc(m))-tetrofosmin was prepared using four different reconstitution methods. The radiochemical purity (RCP) of these products was assessed 8 h later using thin layer chromatography (TLC). Material produced using the original method supplied by the manufacturer and using an newer method, which involves the use of a vent needle and the addition of air, had acceptable RCP (mean +/- SD 94.2 +/- 1.1% and 94.7 +/- 1.7%, respectively) and similar chromatograms. In addition, both products showed good clinical efficacy and exhibited normal biodistribution behaviour. Preparing 99Tc(m)-tetrofosmin using the two other methods, one using a high radioactive concentration and the other maintaining the nitrogen content of the kit vial, gave rise to chromatograms with reduced RCP (63.5 +/- 10.9% and 61.9 +/- 7.6%, respectively) and greater levels of impurities. Although neither of these last two preparations was used clinically, we suggest that reports of poor quality images may be the result of administration of materials similar to these. Results for the high radioactive concentration method were as expected and are consistent with the restrictions imposed by the manufacturer. However, results using the last method are surprising and would suggest that the production of good quality 99Tc(m)-tetrofosmin is dependent on the quantity of nitrogen in the kit vial. We believe that the amount of nitrogen removed from the kit vial during the process of reconstitution is critical. If too much nitrogen is present this will result in poor quality material. In practice it is conceivable that there could be occasions when insufficient nitrogen is removed when following the manufacturer's original guidance, thereby leading to low RCP material. To ensure adequate nitrogen is removed during reconstitution, adoption of the manufacturer's revised method, involving the deliberate introduction of air, is therefore appropriate.

No abstract