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Plasma pharmacokinetics, whole-body distribution, metabolism, and radiation dosimetry of 68Ga bombesin antagonist BAY 86-7548 in healthy men.
- Source :
-
Journal of nuclear medicine : official publication, Society of Nuclear Medicine [J Nucl Med] 2013 Jun; Vol. 54 (6), pp. 867-72. Date of Electronic Publication: 2013 Apr 05. - Publication Year :
- 2013
-
Abstract
- Unlabelled: This first-in-human study investigated the safety, tolerability, metabolism, pharmacokinetics, biodistribution, and radiation dosimetry of (68)Ga-bombesin antagonist (68)Ga-DOTA-4-amino-1-carboxymethylpiperidine-d-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2 (BAY 86-7548).<br />Methods: Five healthy men underwent dynamic whole-body PET/CT after an intravenous injection of BAY 86-7548 (138 ± 5 MBq). Besides total radioactivity, plasma samples were analyzed by radio-high-performance liquid chromatography for metabolism of the tracer. Dosimetry was calculated using the OLINDA/EXM software.<br />Results: Three radioactive plasma metabolites were detected. The proportion of unchanged BAY 86-7548 decreased from 92% ± 9% at 1 min after injection to 19% ± 2% at 65 min. The organs with the highest absorbed doses were the urinary bladder wall (0.62 mSv/MBq) and the pancreas (0.51 mSv/MBq). The mean effective dose was 0.051 mSv/MBq. BAY 86-7548 was well tolerated by all subjects.<br />Conclusion: Intravenously injected BAY 86-7548 is safe, and rapid metabolism is demonstrated. A 150-MBq injection of BAY 86-7548 results in an effective dose of 7.7 mSv, which could be reduced to 5.7 mSv with frequent bladder voids.
Details
- Language :
- English
- ISSN :
- 1535-5667
- Volume :
- 54
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- Journal of nuclear medicine : official publication, Society of Nuclear Medicine
- Publication Type :
- Academic Journal
- Accession number :
- 23564761
- Full Text :
- https://doi.org/10.2967/jnumed.112.114082