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[99mTc]Tc-N4-[alpha-Me-Trp8]MJ9

Development stage: Preclinical
Lead developer: University of Patras
Modality: Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptides
Administration: Intravenous

Overview

[99mTc]Tc-N4-[alpha-Me-Trp8]MJ9 is a radiopharmaceutical imaging agent designed for single-photon emission computed tomography (SPECT). It is a derivative of the MJ9 peptide, a bombesin-like peptide antagonist that targets the gastrin-releasing peptide receptor (GRPR). The compound features an alpha-methyl tryptophan substitution at the Trp8 position, which was originally intended to improve metabolic stability for targeted radiotherapy. It is labeled with technetium-99m via a 6-carboxy-1,4,8,11-tetraazaundecane (N4) chelator. Preclinical studies in PC-3 tumor-bearing mice have demonstrated high GRPR affinity and improved pharmacokinetics compared to reference tracers, suggesting potential applications in imaging prostate cancer, breast cancer, and gastrointestinal stromal tumors.

Other names: 99mTc-labeled N4-[alpha-Me-Trp8]MJ9technetium-99m N4-[alpha-methyl-tryptophan8]MJ9

Targets

GRPR (Gastrin-releasing peptide receptor)

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