Development and evaluation of a single domain antibody targeting folate receptor alpha for radioligand therapy.

ABSTRACT:

Background

Folate receptor alpha (FRα) overexpression is seen in many cancers. Radioligand therapy (RLT) has emerged as a promising tool to target FRα and has been investigated previously, but further progression was limited due to high kidney retention and, subsequently, toxicity. To circumvent this, we present here the development of a [¹³¹I]I-GMIB-conjugated anti-human FRα (hFRα) single-domain antibody (sdAb), with intrinsically fast renal clearance and concomitant low kidney retention. We report the hit-to-lead development of an anti-hFRα sdAb. We evaluated its potential in vitro and assessed its targeting ability using SPECT imaging in hFRα-knockin and tumour-bearing mice. The toxicity and therapeutic efficacy of the [¹³¹I]I-GMIB-sdAb were investigated in

SUBMITTER: Dewulf J 

PROVIDER: S-EPMC11656858 | biostudies-literature | 2024 Dec

REPOSITORIES: biostudies-literature