RADIOLABELLED (LYSSup3/Sup)BN-IPSMA FOR THE DUAL RECOGNITION OF THE PSMA AND GRPR PROTEINS IIN VIVO/I

摘要

Human prostate tumours display intrinsic heterogeneity and changes in phenotype as the disease progresses, which involves various levels of cell-surface receptor expression. The invention relates to a new radiolabelled (Lys3)bombesina-iPSMA molecule for the dual recognition of prostate-specific membrane antigen (PSMA) protein and gastrin-releasing peptide receptor (GRPr) protein in vivo, wherein the chemical steric screening of the chelating site of the radio metal promotes increased capture and internalisation in human prostate cancer cells. The new (Lys3)bombesina-iPSMA molecule labelled with a radio metal (for example, Lu-177) is accumulated with high affinity in vivo in tumour cells that overexpress PSMA protein and/or GRPr protein, acting as a heterodimeric radiopharmaceutical agent when it interacts with two different molecular targets. The purpose of the invention is to provide a new radiolabelled heterodimeric molecule having a specific dual molecular recognition (molecular-target radiopharmaceutical) for the diagnosis and potential treatment of tumours with different PSMA and GRPr expression levels.