Peptides labeled with a radionuclide that emits positrons for PET imaging of human uPAR

摘要

A positron-emitting radionuclide-labeled peptide conjugate for use in the prediction / diagnosis of aggressiveness, prognosis, progression or recurrence by PET imaging of tumors expressing uPAR in vivo in humans, said conjugate comprising a coupled uPAR-binding peptide via chelating agent NOTE to a 68Ga radionuclide, in which the conjugate is administered in a dose of 100 - 500 MBq followed by PET scanning ½ - 24 h after the conjugate has been administered, and quantification by SUVmax and / or SUVmedia, in which the peptide is selected from the group consisting of: (D-Asp) - ([beta] -cyclohexyl-L-alanine) - (Phe) - (D-Ser) - (D-Arg ) - (Tyr) - (Leu) - (Trp) - (Ser), (Ser) - (Leu) - ([beta] -cyclohexyl-L-alanine) - (Phe) - (D-Ser) - (Gln ) - (Tyr) (Leu) - (Trp) - (Ser), (D-Glu) - ([beta] -cyclohexyl-L-alanine) - (Phe) - (D-Ser) - (D-Tyr) - (Tyr) - (Leu) - (Trp) - (Ser), (Asp) - ([beta] -cyclohexyl-L-alanine) - (Phe) - (D-Ser) - (D-Arg) - ( Tyr) - (Leu) - (Trp) - (Ser), (Asp) - ([beta] -ci chlohexyl-L-alanine) - (Phe) - (Ser) - (D-Arg) - (Tyr) -Leu) - (Trp) - (Ser), (D-Asp) - ([beta] -cyclohexyl-L -alanine) - (Phe) - (Ser) - (D-Arg) - (Tyr) -Leu) - (Trp) - (Ser), (D-Thr) - ([beta] -cyclohexyl-L-alanine) - (Phe) - (D-Ser) - (D-Arg) - (Tyr) - (Leu) - (Trp) - (Ser), (D-Asp) - ([beta] -cyclohexyl-L-alanine) - (Phe) - (D-Ser) - (D-Arg) - (Tyr) - (Leu) - ([beta] -2-naphthyl-L-alanine) - (Ser), (Asp) - ([beta ] -cyclohexyl-L-alanine) - (Phe) - (D-Ser) - (Arg) - (Tyr) - (Leu) - (Trp) - (Ser), (Asp) - ([beta] -cyclohexyl- L-Alanine) - (Phe) - (D-Ser) - (D-Arg) - (Tyr) - (Leu) ([beta] -1-naphthyl-L-Alanine) - (Ser), (D-Glu ) - ([beta] -cyclohexyl-L-alanine) - (Phe) - (D-Ser) - (Tyr) - (Tyr) - (Leu) - (Trp) - (Ser), (Asp) - ([ beta] -cyclohexyl-L-alanine) - (Phe) - (D-Ser) - (D-Arg) - (Leu) - (Leu) - (Trp) - (D-His), (Asp) - ([ beta] -cyclohexyl-L-alanine) - (Phe) - (D-Ser) - (D-Arg) - ([beta] -cyclohexyl-L-alanine) - (Leu) - (Trp) - (Ile), (Asp) - ([beta] -cyclohexyl-L-alanine) - (Phe) - (D-Ser) - (D-Arg) - (Tyr) - (Leu) ([beta] -1-naphthyl-L- alanine) - (D-His), (Asp) - ([beta] -cyclohexyl-L-alanine) - (Phe) - (D-Ser) - (D-Arg) - (N- (2,3-dimethoxybenzyl ) glycine) - (D-Phe ) - (N- (3- indolylethyl) glycine) - (N- (2-methoxyethyl) glycine), (Asp) - ([beta] -cyclohexyl-L-alanine) - (Phe) - (D-Ser) - (D-Arg) - (N- (2,3-dimethoxybenzyl) glycine) - (D-Phe) - (N-benzylglycine) - (N- (2 [beta] methoxyethyl) glycine), (Asp) - ([ beta] -cyclohexyl-L-alanine) - (Phe) - (D-Ser) - (D-Arg) - (N- (2,3-dimethoxybenzyl) glycine) - (D-Phe) - (N- (methylnaphthalyl) ) glycine) - (N- (2-methoxyethyl) glycine), and (Asp) - ([beta] -cyclohexyl-L-alanine) - (Phe) - (D-Ser) - (D-Arg) - (N - (2,3-dimethoxybenzyl) glycine) - (D-Phe) - (N- (2,3-dimethoxybenzyl) glycine) - (Ile) wherein the C-terminus is either a carboxylic acid or an amide.