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Review
. 2023 Jul;18(3):419-428.
doi: 10.1016/j.cpet.2023.02.007. Epub 2023 Apr 6.

Fibroblast Activation Protein Inhibitor Theranostics: Early Clinical Translation

Yuriko Mori  1 , Clemens Kratochwil  2 , Uwe Haberkorn  2 , Frederik L Giesel  3
Affiliations
Review

Fibroblast Activation Protein Inhibitor Theranostics: Early Clinical Translation

Yuriko Mori et al. PET Clin. 2023 Jul.

Abstract

Fibroblast activation protein (FAP)-targeted radioligand therapy offers a possibility of a novel cancer therapeutic strategy, aiming at tumor stroma1. Early clinical translations of FAP-tracers occurred as early as in the 1990s using antibodies, without substantial achievement further than the clinical phase II trial. The essential step toward the theranostic approach, with a conceptual combination of diagnostic and therapeutic emitters in a specific tracer, began with the implementation of small-molecule FAP-enzyme inhibitors (FAPI) in 2018. Currently, FAPI-04 and FAPI-46, containing DOTA-chelators with the possibility of radionuclide combination (Ga-68, Y-90, and Lu-177), are the compounds most widely used in the theranostic regimen.

Keywords: Clinical translation; FAPI; Fibroblast; Radioligand therapy; Theranostic.

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