Synthesis, proteolytic stability, and in vitro evaluation of DOTA conjugated p160 peptide based radioconjugates: [177Lu]Lu–DOTA–p160

Abstract

In this work, we describe the synthesis, in vitro stability, and preliminary biological evaluation of [¹⁷⁷Lu]Lu–DOTA–p160 peptide-based radiopharmaceuticals. Our findings highlight that all DOTA–p160–peptide radioconjugates exhibit favorable proteolytic and enzymatic stability with a prolonged half-life in human plasma and serum. Cell uptake studies carried out on MCF-7 cell line revealed saturable binding of the radioconjugates in the nanomolar range, thereby demonstrating their promising potential in the imaging and therapy of breast tumors.