Preclinical evaluation of FAP-2286 for fibroblast activation protein targeted radionuclide imaging and therapy.

ABSTRACT:

Purpose

Fibroblast activation protein (FAP) is a membrane-bound protease that has limited expression in normal adult tissues but is highly expressed in the tumor microenvironment of many solid cancers. FAP-2286 is a FAP-binding peptide coupled to a radionuclide chelator that is currently being investigated in patients as an imaging and therapeutic agent. The potency, selectivity, and efficacy of FAP-2286 were evaluated in preclinical studies.

Methods

FAP expression analysis was performed by immunohistochemistry and autoradiography on primary human cancer specimens. FAP-2286 was assessed in biochemical and cellular assays and in in vivo imaging and efficacy studies, and was further evaluated against FAPI-46, a small molecule-based FAP-targeting agent.

Results

Immunohis

SUBMITTER: Zboralski D 

PROVIDER: S-EPMC9399058 | biostudies-literature | 2022 Sep

REPOSITORIES: biostudies-literature