Selenium-75-labeled sucralfate: comparison with other radiolabels and initial clinical studies

Area of Science:

• Gastroenterology
• Radiopharmacology
• Biomedical Imaging

Background:

• Sucralfate is a medication used to treat ulcers.
• Developing stable radiolabeled sucralfate is crucial for diagnostic imaging of gastrointestinal conditions.

Purpose of the Study:

• To synthesize and evaluate 75Se-sucralfate for stability and efficacy in imaging gastrointestinal lesions.
• To compare the performance of 75Se-sucralfate with 111In-sucralfate and 99mTc-HSA-sucralfate.

Main Methods:

• Synthesis of 75Se-sucralfate and comparison with 111In-sucralfate and 99mTc-HSA-sucralfate in vitro and in an animal ulcer model.
• In vitro stability testing in human gastric juice and simulated intestinal fluid.
• Biodistribution studies in rats and imaging studies in patients with esophagitis, gastritis, and gastric ulcers.

Main Results:

• 75Se label exhibited superior stability in gastric and intestinal fluids compared to 111In and 99mTc-HSA labels.
• In rats with gastric ulcers, 75Se-sucralfate showed significantly higher ulcer-to-nonulcer radioactivity ratios.
• Selective binding of 75Se-sucralfate was successfully imaged in patients with esophagitis, gastritis, and gastric ulcers, but not duodenal ulcers.

Conclusions:

• 75Se-sucralfate is a stable and effective radiotracer for imaging gastric lesions.
• The tracer demonstrates selective binding to ulcer sites and is minimally absorbed from the GI tract.
• Further investigation may be warranted for imaging other gastrointestinal conditions.