Prostate cancer is one of the most common malignancies in men, and the prostate-specific membrane antigen (PSMA) has emerged as a key molecular target for imaging and targeted radionuclide therapy (TRT). However, current PSMA-targeted radiopharmaceuticals often display rapid blood clearance and high renal uptake, which can limit their therapeutic performance. This work focused on the design, synthesis, and preclinical evaluation of a novel heterobivalent radiocomplex aimed at improving the pharmacokinetic properties of PSMA-targeted agents. The developed conjugate, DOTA–IPBA–PEG–PSMA, integrates a PSMA-binding moiety with an albumin-binding unit, 4-(p-iodophenyl)butyric acid (IPBA), to promote a reversible interaction with serum albumin. This dual-targeting strategy was intended to prolong systemic circulation and enhance tumor accumulation while minimizing non-specific uptake.