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Published on: January 7, 2019
Human urinary excretion of NC100692, an RGD-peptide for imaging angiogenesis
L Roed1, I Oulie, B J McParland
1Research and Development, GE Healthcare, Nycoveien 2, N-0485 Oslo, Norway. line.roed@ge.com
Summary
Human urine analysis revealed only intact NC100692, not metabolites, after (99m)Tc-NC100692 injection. Most of the diagnostic agent was excreted within the first hour.
Area of Science:
- Nuclear medicine
- Radiopharmacology
- Analytical chemistry
Background:
- NC100692 is a technetium-99m ((99m)Tc) complex investigated for detecting angiogenesis.
- Previous studies in rats indicated the presence of NC100692 metabolites in urine.
Purpose of the Study:
- To analyze human urine samples for intact NC100692 and its metabolites after intravenous administration.
- To compare human metabolic profiles with previously observed rat data.
Main Methods:
- Reversed-phase liquid chromatography coupled with ion-trap mass spectrometry (LC-MS) was used.
- Analysis was performed on urine samples from a Phase I clinical study following (99m)Tc-NC100692 injection.
Main Results:
- Only intact NC100692 was detected in human urine; no metabolites were found.
- Approximately 30% of the injected dose was excreted within 4-8 hours, with most in the first hour.
- NC100692 accounted for 98% of the total urinary (99m)Tc recovery in the first hour, suggesting excretion as the intact complex.
Conclusions:
- Human metabolism of (99m)Tc-NC100692 differs significantly from rats, with no detectable metabolites in urine.
- (99m)Tc-NC100692 is primarily excreted unchanged in human urine.
- The diagnostic agent shows stability in humans, with rapid urinary excretion of the intact complex.
