Evans blue-modified radiolabeled fibroblast activation protein inhibitor as long-acting cancer therapeutics.

ABSTRACT: Rationale: Fibroblast activation protein (FAP) targeted molecular imaging radiotracers have shown promising preclinical and clinical results in tumor diagnosis. However, rapid clearance and inadequate tumor retention of these molecules have hindered them for further clinical translation in cancer therapy. In this study, we aimed to develop a series of albumin binder-truncated Evans blue (EB) modified FAP targeted radiotracers, and optimize the pharmacokinetic (PK) characteristics to overcome the existing limitations in order to apply in the radionuclide therapy of cancer. Methods: A series of compounds with the general structure of EB-FAPI-Bn were synthesized based on a FAP inhibitor (FAPI) variant (FAPI-02) and radiolabeled with ¹⁷⁷LuCl₃. To verify the

SUBMITTER: Wen X 

PROVIDER: S-EPMC8690933 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature