Overview of Development and Formulation of ¹⁷⁷Lu-DOTA-TATE for PRRT

Current Radiopharmaceuticals
Wouter A P BreemanErik de Blois

Abstract

Peptide receptor radionuclide therapy (PRRT) using radiolabeled somatostatin analogs has become an established procedure for the treatment of patients suffering from inoperable neuroendocrine cancers over-expressing somatostatin receptors. Success of PRRT depends on the availability of the radiolabeled peptide with adequately high specific activity, so that required therapeutic efficacy can be achieved without saturating the limited number of receptors available on the target lesions. Specific activity of the radionuclide and the radiolabeled somatostatin analog are therefore an important parameters. Although these analogs have been investigated and improved, and successfully applied for PRRT for more than 15 years, there are still many possibilities for further improvements that fully exploit PRRT with 177Lu-DOTA-TATE. The here summarized data presented herein on increased knowledge of the components of 177Lu-DOTA-TATE (especially the purity of 177Lu and specific activity of 177Lu) and the reaction kinetics during labeling 177Lu-DOTA-TATE clearly show that the peptide dose and dose in GBq can be varied. Here we present an overview of the development, formulation and optimisation of 177Lu-DOTA-TATE, mainly addressing radiochemi...Continue Reading

Citations

May 22, 2016·European Journal of Nuclear Medicine and Molecular Imaging·Christian H PfobMatthias Eiber
Sep 13, 2017·Dalton Transactions : an International Journal of Inorganic Chemistry·Z LiuE Oehlke

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