Optimizing labelling conditions of ²¹³Bi-DOTATATE for preclinical applications of peptide receptor targeted alpha therapy.

ABSTRACT:

Background

²¹³Bismuth (²¹³Bi, T_1/2 = 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 MBq ²²⁵Ac (actinium), due to limited availability and the high cost to produce large-scale ²²⁵Ac/²¹³Bi generators, might complicate in vitro and in vivo applications though.Here we present optimized labelling conditions of a DOTA-peptide with an ²²⁵Ac/²¹³Bi generator (< 222 MBq) for preclinical applications using DOTA-Tyr³-octreotate (DOTATATE), a somatostatin analogue. The following labelling conditions of DOTATATE with ²¹³Bi

SUBMITTER: Chan HS 

PROVIDER: S-EPMC5843812 | biostudies-literature | 2017

REPOSITORIES: biostudies-literature