Enhanced Radionuclide Therapy via the Conjugation of Pentadecanoic Acids With ²²⁵Ac- and ¹⁷⁷Lu-Labeled RGD Peptides.

ABSTRACT: Improved peptide pharmacokinetics are needed to enhance the therapeutic effects of peptide-based radionuclide therapy. Conjugation of albumin binders, such as fatty acids, to tumor-targeting peptides slows blood clearance, resulting in higher tumor uptake. In this study, we synthesized PD-conjugated monomeric and dimeric RGD peptides, PD-K-(¹¹¹In-DOTA)-c(RGDfK) and PD-K(¹¹¹In-DOTA)-E[c(RGDfK)]₂, and evaluated their albumin binding. We compared pharmacokinetics with and without PD in tumor-bearing mice. The therapeutic effects of PD-K(¹⁷⁷Lu-DOTA)-c(RGDfK) (7.5, 15, and 30 MBq) and PD-K(²²⁵Ac-DOTA)-c(RGDfK) (20 and 40 kBq) were investigated in tumor-bearing mice. ¹⁷⁷Lu-DOTA-c(RGDfK) (30 MBq) was used as a control to evaluate t

SUBMITTER: Yoshimoto M 

PROVIDER: S-EPMC12775587 | biostudies-literature | 2026 Jan

REPOSITORIES: biostudies-literature