Radiometal-Labelled Macrocyclic Chelator-Derivatised Somatostatin Analogue with Superb Tumour-Targeting Properties and Potential for Receptor-Mediated Internal Radiotherapy
A. Heppeler(University Hospital of Basel), Sylvie Froidevaux, Helmut R. Mäcke(University Hospital of Basel), E. Jermann(University Hospital of Basel), Martin Béhé(University Hospital of Basel), P. Powell(University Hospital of Basel), Michael Hennig(Roche (Switzerland))
Chemistry - A European Journal
July 2, 1999
Cited by 334
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.
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