Radiometal-Labelled Macrocyclic Chelator-Derivatised Somatostatin Analogue with Superb Tumour-Targeting Properties and Potential for Receptor-Mediated Internal Radiotherapy

A. Heppeler, Sylvie Froidevaux, Helmut R. Mäcke, E. Jermann, Martin Béhé, P. Powell, Michael Hennig

Chemistry - A European Journal · 1999 · 334 citations · 0 references

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Abstract

A highly stable octacoordinated Y-DOTA-D-Phe-amide (see picture) allows the first use of the powerful β-emitter 90Y, coupled to a bioactive peptide, in internal radiotherapy of cancer. The same peptide labelled with the γ-emitter, 67Ga, shows improved biodistribution as a consequence of the hexacoordination of the GaIII complex with a pendant, ionised, acetic acid group.