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

MerLion Pharma (Germany) · Clovis Oncology (United States) · +1 more institution

PubMed
Indexed incrossrefpubmed

Abstract

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…

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252
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21.94
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100%
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50
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Authors

21

Topics & keywords

Keywords
  • Fibroblast activation protein, alpha
  • Radionuclide therapy
  • Medicine
  • Radionuclide imaging
  • Nuclear medicine
  • Medical physics
  • Internal medicine
  • Cancer
UN Sustainable Development Goals
  • Good health and well-being
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