Structurally-Optimized Peptide VMT-Alpha-NET Enhances the Efficacy of SSTR2-Targeted Alpha-Particle Therapy for Neuroendocrine Tumors

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Introduction: 203Pb/212Pb is a promising theranostics pair for SSTR2-targeted alpha-particle therapy for neuroendocrine tumors (NETs). The development of SSTR2-targeted peptides that are optimized for the Pb isotopes has the potential to improve performance.

Aim(s): The aim of the study was to evaluate the potential of a new peptide structure, VMT-alpha-NET for 203Pb/212Pb theranostics.

Materials and methods: DOTA-tyr3-octreotide (DOTATOC) and VMT-alpha-NET were synthesized, and the binding affinity and cellular uptake were evaluated in AR42J cells. Biodistribution and imaging studies using AR42J tumor-bearing mice were conducted using 203Pb as a surrogate of 212Pb. 212Pb therapy and ongoing studies to evaluate potential toxicities demonstrate the potential of the new peptide.

Conference: 17th Annual ENETSConcerence (2020)

Presenting Author:

Authors: Lee D, Li M, Baumhover N, Liu D, Sagastume E,

Keywords: prrt, VMT-alpha-NET, 203Pb/212Pb theranostics,