Radiolabelled somatostatin analogues have been used in diagnostic and thera
peutic nuclear medicine to treat cancerous tumours. Lanreotide, a cyclic oc
tapeptide, beta -naphthyl-peptide, with antiproliferative action on human s
mall cell lung carcinoma was Re-188 labelled and characterised, and its bio
distribution was studied in mice. Molecular modelling indicates that the li
pophilic radiopharmaceutical might be an oxo-rhenium (V) penta-coordinated
complex. The implanted human cervical tumour of epidermoid origin was posit
ive for cytokeratins and Vimentin. Uptake of Re-188-labelled peptide in the
implanted tumour in athymic mice was 6.2+/-2.9% and was rapidly cleared vi
a the hepatobiliary system. Re-188-beta -naphthyl-peptide might be a potent
ial therapeutic agent. (C) 2001 Elsevier Science Inc. All rights reserved.