Prostate-specific membrane antigen (PSMA) is a transmembrane glycoprotein highly expressed in many prostate cancers, and can be targeted with radiolabeled antibodies for diagnosis and treatment of this disease. To serve as a radioimmunotherapeutic agent, a kinetically inert conjugate is desired to maximize tumor uptake and tumor radiation dose with minimal nonspecific exposure to bone marrow and other major organs. In this study, we assessed the pharmacokinetics and biodistribution of the 7E11 monoclonal antibody (MAb) radiolabeled with the lutetium-177 ( 177 Lu) -tetraazacyclododecanetetraacetic acid (DOTA) conjugate system ( 177 Lu-7E11) versus those of the 7E11 MAb radiolabeled with the indium-111 ( 111 In) -glycyl-tyrosyl-(N,-diethylenetriaminepentaacetic acid)-lysine hydrochloride (DTPA) conjugate system ( 111 In-7E11, also known as ProstaScint ® ), to determine the feasibility of using 111 In-7E11 as a pretherapeutic agent for 177 Lu-7E11 radioimmunotherapy. Pharmacokinetic and biodistribution studies of 177 Lu-7E11 in LNCaP xenograft mice were performed at 2, 8, 12, 24, 72, and 168 hours after radiopharmaceutical administration. For 111 In-7E11, pharmacokinetic and biodistribution studies were performed at 8, 24, and 72 hours. Parallel studies of 177 Lu-7E11 in nontumor bearing mice at 8, 24, and 72 hours postinjection served as controls. Gamma scintigraphy was performed, followed by autoradiography and tissue counting to demonstrate and quantify the distributions of radioconjugated MAb in the tumor and normal tissues. Both 177 In-7E11 conjugates demonstrated an early blood pool phase in which uptake was dominated by the blood, lung, spleen and liver, followed by uptake and retention of the radiolabeled antibody in the tumor which was most prominent at 24 h. Total accumulation of radioconjugated MAb in tumor at 24 h was greater in the case of 177 Lu-7E11 in comparison to that of 111 In-7E11. Continued accumulation in tumor was observed for the entire time course studied for both 177 Lu-7E11 and 111 In-7E11. The liver was the only major organ demonstrating a significant difference in accumulation between the two conjugates. In conclusion, pharmacokinetic and biodistribution studies of 177 Lu-7E11 in LNCaP xenograft mouse models support its potential application as a radioimmunotherapeutic agent targeting prostate cancer, and the distribution and tumor uptake of 111 In-7E11 appear to be similar to those of 177 Lu-7E11, supporting its use as a pretherapeutic tool to assess the potential accumulation of 177 Lu-7E11 radioimmunotherapeutic at sites of prostate cancer. However, the different accumulation patterns of the 111 In and 177 Lu immunoconjugates in liver will likely prevent the use of 111 In-7E11 as a true dosimetry tool for 177 Lu-7E11 radioimmunotherapy.