Although targeting significantly improved tumour retention and tissue penetration of both nanocarriers in PSMA-positive PC3-Pip xenografts, the multivalent nanocarrier [89Zr]PEG-(DFB)1(ACUPA)3 bearing three ACUPA ligands showed a remarkably higher PC3-Pip/blood ratio and background clearance. The gene discussed is PIP; the disease is neoplasm.