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[99mTc]Tc-N4-asp-[Bta8]MJ9
- Development stage
- Unknown
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptides
- Administration
- Intravenous
01
Overview
[99mTc]Tc-N4-asp-[Bta8]MJ9 is a technetium-99m labeled radiopharmaceutical imaging agent developed for SPECT/CT visualization of tumors expressing the gastrin-releasing peptide receptor (GRPR). The compound is a bombesin-based peptide derivative derived from the MJ9 peptide sequence (H-Pip5-phe6-Gln7-Trp8-Ala9-Val10-Gly11-His12-Sta13-Leu14-NH2), featuring a specific substitution of tryptophan at position 8 with β-(3-benzothienyl) alanine (Bta8). This modification is intended to optimize pharmacokinetics by reducing accumulation in healthy GRPR-positive organs such as the pancreas and stomach, thereby improving tumor-to-background contrast. The peptide is conjugated to a 6-carboxy-1,4,8,11-tetraazaundecane (N4) chelator via an aspartic acid linker. It targets GRPR, which is frequently overexpressed in various malignancies, including prostate cancer, breast cancer, and gastrointestinal stromal tumors. Preclinical studies have demonstrated high receptor affinity and favorable imaging properties, and clinical translation has been initiated.
- Other names
- 99mTc-labeled N4-asp-[Bta8]MJ9N4-asp-[Bta8]MJ9
02
Targets
GRPR (Gastrin-releasing peptide receptor)
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