Pretargeted Alpha Therapy of Disseminated Cancer Combining Click Chemistry and Astatine-211.

ABSTRACT: To enhance targeting efficacy in the radioimmunotherapy of disseminated cancer, several pretargeting strategies have been developed. In pretargeted radioimmunotherapy, the tumor is pretargeted with a modified monoclonal antibody that has an affinity for both tumor antigens and radiolabeled carriers. In this work, we aimed to synthesize and evaluate poly-L-lysine-based effector molecules for pretargeting applications based on the tetrazine and trans-cyclooctene reaction using ²¹¹At for targeted alpha therapy and ¹²⁵I as a surrogate for the imaging radionuclides ^{123, 124}I. Poly-L-lysine in two sizes was functionalized with a prosthetic group, for the attachment of both radiohalogens, and tetrazine, to allow binding to the trans-cyclooctene-modified pretargeti

SUBMITTER: Timperanza C 

PROVIDER: S-EPMC10145095 | biostudies-literature | 2023 Apr

REPOSITORIES: biostudies-literature