Optimizing labelling conditions of213 Bi-DOTATATE for preclinical applications of peptide receptor targeted alpha therapy

EJNMMI Radiopharmacy and Chemistry
Ho Sze ChanWouter A P Breeman

Abstract

213 Bismuth (213Bi, T1/2= 45.6 min) is one of the most frequently used α-emitters in cancer research. High specific activity radioligands are required for peptide receptor radionuclide therapy. The use of generators containing less than 222 MBq225Ac (actinium), due to limited availability and the high cost to produce large-scale225Ac/213Bi generators, might complicate in vitro and in vivo applications though.Here we present optimized labelling conditions of a DOTA-peptide with an225Ac/213Bi generator (< 222 MBq) for preclinical applications using DOTA-Tyr3-octreotate (DOTATATE), a somatostatin analogue. The following labelling conditions of DOTATATE with213Bi were investigated; peptide mass was varied from 1.7 to 7.0 nmol, concentration of TRIS buffer from 0.15 mol.L-1to 0.34 mol.L-1, and ascorbic acid from 0 to 71 mmol.L-1in 800 μL. All reactions were performed at 95 °C for 5 min. After incubation, DTPA (50 nmol) was added to stop the labelling reaction. Besides optimizing the labelling conditions, incorporation yield was determined by ITLC-SG and radiochemical purity (RCP) was monitored by RP-HPLC up to 120 min after labelling. Dosimetry studies in the reaction vial were performed using Monte Carlo and in vitro clonogenic ass...Continue Reading

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Citations

Aug 15, 2019·Journal of Labelled Compounds & Radiopharmaceuticals·Anzhelika YakushevaStepan Kalmykov
Jul 23, 2019·EJNMMI Radiopharmacy and Chemistry·BioMed Central
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Related Concepts

Acids
Actinium
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