University of Bern

Klaus-Peter Eisenwiener

Helmut Robert Maecke

Hans Rink

In one embodiment, a method for treating a cancerous disease is provided which includes characterizing a disease by an overexpression of one or more somatostatin receptors, and exposing the one or more somatostatin receptors to a pharmaceutical composition comprising a somatostatin analogue which binds to the one or more somatostatin receptors. In one example, the somatostatin analogue may have the general formula: wherein Z is optionally present or absent and when present is selected from the group consisting of DOTA-based chelators, DTPA-based chelators, NOTA-based chelators, carbonyl compounds, hydrazino nicotinamide, N4-chelators, desferrioxamine, NS-chelators, tyrosine for halogenation, a fluorescent dye, and biotin; L is optionally present or absent and when present is a linker molecule; X1 is a symmetric or asymmetric diamino acid containing 3 or 4 consecutive carbon atoms; X2 is a positively charged natural or unnatural amino acid, an arginine mimic, citrulline, or a neutral amino acid; X3 is phenylalanine, Ala-[3-(2-thienyl)], &#x3b1;-naphthylalanine, or &#x3b2;-naphthylalanine; X4 is an aromatic amino acid; X5 is threonine or serine; and X6 is phenylalanine, Ala-[3-(2-thienyl)], &#x3b1;-naphthylalanine, or &#x3b2;-naphthylalanine.

Treatment process using somatostatin analogues

In one embodiment, a composition of somatostatin analogues having the general formula: is provided wherein Z may be absent or present and when present is selected from DOTA- and DTPA-based chelators, NOTA-based chelators, carbonyl compounds, hydrazino nicotinamide, N-chelators, desferrioxamine, NS-chelators, optionally complexed or labeled with a radioisotope, tyrosine for halogenation, a fluorescent dye, or biotin. The composition further provides that L may or may not be present and when present is a linker molecule, X1 is glutamic acid or a symmetric or asymmetric diamino acid containing 3 or 4 consecutive C atoms, X2 is a positively charged natural or unnatural amino acid, an arginine mimic, citrulline, or a neutral amino acid, X3 is phenylalanine, Ala-[3-(2-thienyl)], &#x3b1;-naphthylalanine, or &#x3b2;-naphthylalanine, X4 is an aromatic amino acid, X5 is threonine or serine, and X6 is phenylalanine, Ala-[3-(2-thienyl)], &#x3b1;-naphthylalanine, or &#x3b2;-naphthylalanine.

Growing community of inventors

Bern, Switzerland

Klaus-Peter Eisenwiener