Related Experiment Video
Updated: Jul 7, 2026
08:47
Protocol for Isolation of Primary Human Hepatocytes and Corresponding Major Populations of Non-parenchymal Liver Cells
Published on: March 30, 2016
36.9K
First-in-Human Serum Stability Studies of [177Lu]Lu-AMTG: A Step Toward Improved GRPR-Targeted Radiopharmaceutical
Veronika Felber1, Nadine Holzleitner1, Markus Joksch2
1Department of Chemistry, TUM School of Natural Sciences, Technical University of Munich, Garching, Germany.
Summary
The novel radiotracer [177Lu]Lu-AMTG shows high in vivo serum stability in humans, exceeding that of [68Ga]Ga-RM2. This finding supports its potential for improved radiopharmaceutical therapy in GRPR-expressing cancers.
Area of Science:
- Nuclear medicine
- Radiopharmaceutical chemistry
- Oncology
Background:
- Gastrin-releasing peptide receptor (GRPR) targeted PET/CT using [68Ga]Ga-AMTG can detect metastatic disease missed by [18F]PSMA PET/CT in metastatic castration-resistant prostate cancer.
- Preclinical studies indicated high stability for AMTG compounds.
Purpose of the Study:
- To assess the in vivo serum stability of [177Lu]Lu-AMTG in human subjects.
- To evaluate the therapeutic potential of [177Lu]Lu-AMTG.
Main Methods:
- Intravenous injection of 7.6 ± 0.1 GBq of [177Lu]Lu-AMTG.
- Collection of blood samples at various time points post-injection.
- Analysis of serum samples using reversed-phase high-performance liquid chromatography.
Main Results:
- The in vivo serum stability of [177Lu]Lu-AMTG at 1 hour post-injection was significantly higher (62% ± 6%) compared to [68Ga]Ga-RM2 (19% ± 2%).
Conclusions:
- [177Lu]Lu-AMTG exhibits high in vivo serum stability in humans.
- Favorable biodistribution and stability suggest AMTG derivatives hold promise for enhancing radiopharmaceutical therapy in GRPR-expressing malignancies.
