Abstract: A PSMA-targeting conjugate or a pharmaceutically acceptable salt which may be used either for preparing a radiopharmaceutical or, once labeled with a radionuclide, as a radiopharmaceutical. The conjugate is of formula (I): A1-L1-Ch-L2-A2 (I) wherein: Ch is a chelator, L1 and L2, identical or different, are a linker whereas A1 and A2, identical or different, are a urea-based PSMA ligand.

Abstract: A conjugate or a pharmaceutically acceptable salt thereof, the conjugate being of formula: C-L-A, wherein C is a chelator, L is a linker covalently bound to the chelator and A is a Gastrin-releasing peptide receptor antagonist covalently bound to the linker, wherein: the chelator is of formula: where the dotted line represents the covalent bond to the linker; the linker is of formula: -?-Ala-?-Ala-; and the Gastrin-releasing peptide receptor antagonist has the amino acid sequence: -DPhe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2.

Abstract: A process is for preparing a site-specific bioconjugated antibody of a formula (I): Ab-(Linker-Chelator)n (I). The Linker is an oligopeptide with an N-terminal end. The Chelator is a metal chelating agent. n is a Chelator-to antibody ratio (CAR), wherein 0<n?2. The process includes enzymatic deglycosylation of the antibody; coupling of the obtained deglycosylated antibody with a compound of a formula (A): Linker-Chelator (A) in the presence of a transglutaminase. The Linker is bound to the Ab at its N-terminal end, and comprising a sequence chosen among (*G-G-G), (*K-G-G) and (*A-K-A), where * denotes the N-terminal end of the Linker which is covalently bound to the Ab.

Abstract: A cancer targeting composition, kit, and method for treatment of cancer cells overexpressing somatostatin receptors is disclosed. The composition includes a radioisotope, a chelator, and a targeting moiety. The chelator includes a nitrogen ring structure including a tetraazacyclododecane, a triazacyclononane, and/or a tetraazabicyclo [6.6.2] hexadecane derivative. The targeting moiety includes a somatostatin receptor targeting peptide. The somatostatin receptor targeting peptide includes an octreotide derivative. The targeting moiety is chelated to the radioisotope by the chelator whereby the cancer cells are targeted for elimination.

Abstract: A cancer targeting composition, kit, and method for treatment of cancer cells overexpressing somatostatin receptors is disclosed. The composition includes a radioisotope, a chelator, and a targeting moiety. The chelator includes a nitrogen ring structure including a tetraazacyclododecane, a triazacyclononane, and/or a tetraazabicyclo [6.6.2] hexadecane derivative. The targeting moiety includes a somatostatin receptor targeting peptide. The somatostatin receptor targeting peptide includes an octreotide derivative. The targeting moiety is chelated to the radioisotope by the chelator whereby the cancer cells are targeted for elimination.