Despite the progress in the diagnosis and management of early stage disease, the management of advanced prostate cancer remains an important problem. Prostate tissue expresses folate receptor (FR) which binds both folic acid and folate-linked drugs or imaging agents. Doxorubicin is the best known and most widely used member of the anthracycline antibiotic group of anticancer agents. The aim of this work is to develop a multifunctional nanoconjugate, Tc-99m-folate-PEG-doxorubicin, in order to investigate its radiopharmaceutical potential as a prostate cancer imaging and real-time drug location imaging agent. Through this aim, biodistribution studies of Tc-99m-folate-PEG-doxorubicin and control groups (Tc-99m-doxorubicin and Tc-99m-PEG-doxorubicin) in male rats were carried out. Obtained data showed that uptake of Tc-99m-folate-PEG-doxorubicin in prostate was significantly higher than that of the control groups due to the affinity of folate ligand to folate receptor. As a consequence, it was indicated that Tc-99m-FOL-PEG-DOX radiolabeled conjugate which has a great target/non-target organ ratio, is specific for target organ and has a high radiopharmaceutical potential as a prostate cancer and real-time drug location imaging agent.