TY - JOUR T1 - Reduction of Renal Uptake of Radiolabeled Octreotate by Amifostine Coadministration JF - Journal of Nuclear Medicine JO - J Nucl Med SP - 749 LP - 753 DO - 10.2967/jnumed.111.098665 VL - 53 IS - 5 AU - Marleen Melis AU - Roelf Valkema AU - Eric P. Krenning AU - Marion de Jong Y1 - 2012/05/01 UR - http://jnm.snmjournals.org/content/53/5/749.abstract N2 - Megalin-mediated renal retention of radiolabeled somatostatin analogs may lead to nephrotoxicity during peptide receptor radionuclide therapy (PRRT). The cytoprotective agent amifostine protected rats from long-term nephrotoxicity after PRRT with 177Lu-DOTA,Tyr3-octreotate. This study describes the direct effect of amifostine on kidney and tumor uptake of 111In-DOTA,Tyr3-octreotate. Methods: In vivo biodistribution studies were performed using CA20948 tumor–bearing rats, with or without amifostine coadministration, via several routes. In vitro uptake was studied in somatostatin receptor–expressing CA20948 and megalin or cubilin receptor–expressing BN-16 cells, in the absence or presence of amifostine or its active metabolite WR-1065. Results: Coadministration of amifostine decreased renal uptake of radiolabeled octreotate in vivo, whereas tumor uptake was not affected. In agreement, amifostine and WR-1065 coincubation reduced uptake in BN-16 but not in CA20948 cells. Conclusion: Amifostine may provide renal protection during PRRT using somatostatin analogs, both by mitigation of radiation damage and the currently observed reduction of absorbed kidney radiation dose. ER -