The introduction of multiple negative charges into [177Lu]Lu-1 clearly affected renal accumulation leading to a suboptimal biodistribution profile, whereas the combined use of the receptor-specific sequence “Trp-(N-Me)Nle-Asp-1Nal-NH2”of DOTA-MGS5 and a non-charged hydrophilic linker in [177Lu]Lu-2 led to a further enhancement in tumor uptake and favorable tumor-to-organ ratios, confirming the high potential of this new class of radiolabeled MG analogs for therapeutic use in CCK2R-expressing malignancies. The gene discussed is CCKBR; the disease is neoplasm.