Preclinical Development of 3BP-3940, a Fibroblast Activation Protein-Targeted Cyclic Peptide-Based Radiotheranostic

Dirk Zboralski1, Frank Osterkamp2, Jan L von Hacht2

  • 13B Pharmaceuticals GmbH, Berlin, Germany dirk.zboralski@3b-pharma.com.

Insights

A novel peptide, 3BP-3940, shows high affinity and specificity for Fibroblast Activation Protein (FAP). This agent demonstrates potent tumor growth inhibition and minimal uptake in normal tissues, supporting its use in cancer imaging and therapy.

Area of Science:

  • Oncology
  • Radiopharmaceutical Science
  • Molecular Imaging

Background:

  • Fibroblast Activation Protein (FAP) is a key marker in the tumor microenvironment.
  • Existing FAP inhibitors have shown promise in cancer imaging.
  • FAP-targeting agents are crucial for theranostic applications in oncology.

Purpose of the Study:

  • To introduce and evaluate a novel FAP-targeting peptide, 3BP-3940.
  • To assess the preclinical efficacy and safety of 3BP-3940 for cancer theranostics.
  • To investigate the potential of 3BP-3940 in both diagnostic imaging and therapeutic applications.

Main Methods:

  • Biochemical assays were used to determine the potency and selectivity of 3BP-3940.
  • Biodistribution studies were performed in mice and minipigs.
  • Therapeutic efficacy was evaluated in a preclinical HEK-FAP mouse model.

Main Results:

  • 3BP-3940 demonstrated high affinity and specificity for FAP.
  • Radiolabeled 3BP-3940 (with 177Lu) showed persistent tumor uptake and significant tumor growth inhibition.
  • The agent exhibited minimal off-target uptake in normal tissues across species.

Conclusions:

  • 3BP-3940 is a potent and selective FAP-targeting agent.
  • The preclinical data support the clinical utility of 3BP-3940 for cancer theranostics.
  • 3BP-3940 holds promise for both imaging and radiopharmaceutical therapy in cancer patients.

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