Mallinckrodt, Inc.

Biosynthema Inc.

Jean-Claude Reubi

Jörg Schmitt

Helmut Robert Macke

Wout A Breeman

Ananthachari Srinivasan

Mihaela Ginj

The invention relates to a peptide compound having an improved binding affinity to somatostatin receptors, comprising a somatostatin analogue as the peptide and a chelating group covalently linked to the N-terminal free amino group of said peptide, wherein said somatostatin analogue carries an 1-naphthylalanine or a 3-benzothienylalanine residue in its 3-position. The invention further relates to said peptide compound labeled with a detectable element or with a therapeutic radionuclide, as well as to a diagnostic method and to a method for the therapeutic treatment of tumors, by using the labeled compounds.

Peptide compounds having improved binding affinity to somatostatin receptors

Compounds and methods for the diagnosis and treatment of tumors, including breast and prostate tumors and metastases thereof using radiolabelled peptides that bind to GRP receptors. The peptides are Bombesin analogs wherein the first and optionally the third amino acid are modified.

Radiolabeled peptides for the diagnosis and treatment of breast and prostate tumors and metastases of such tumors

The invention relates to a method of detecting and localizing malignant tumors and their metastases in tissues, which in healthy condition and in non-neoplastic conditions of chronic inflammation do not contain substantial quantities of neurotensin-receptors, in the body of a human being, which comprises: (i) administering to said being a composition comprising, in a quantity sufficient for external imaging, a radiolabelled peptide selected from the group consisting of neurotensin (NT), NT-receptor agonists. NT-receptor antagonists, NT analogues and NT derivatives; and thereupon (ii) subjecting said being to external imaging, by radioactive scanning or by magnetic resonance imaging, to determine the targeted sites in the body of said being. The invention further relates to a method for the therapeutic treatment of said malignant tumors by administration of the above-defined peptide, labelled for this purpose, and to the differential-diagnostic assessment and detection of a specific tumor type (i.e. ductal exocrine pancreatic carcinoma) of the pancreas. The invention also relates to a pharmaceutical composition to be used for detection, a pharmaceutical composition to be used for therapy and to a kit for preparing a radiopharmaceutical composition.

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Wabern, Switzerland

Jean-Claude Reubi