In this contribution, we described novel pyrazolyl-diamine Re(I)/99mTc(I) tricarbonyl complexes functionalized with a mitotropic TPP moiety, to promote accumulation of the metal/radiometal in the mitochondria, and with a bombesin analogue (G3BBN[7-14]) for specific recognition of PCa tumor cells overexpressing the GRPr. The gene discussed is GRPR; the disease is neoplasm.