Plasma Pharmacokinetics, Whole-Body Distribution, Metabolism, and Radiation Dosimetry of ^sup 68^Ga Bombesin Antagonist BAY 86-7548 in Healthy Men

• Published in: The Journal of nuclear medicine (1978) Vol. 54; no. 6; p. 867
• Main Authors: Roivainen, Anne, Kähkönen, Esa, Luoto, Pauliina, Borkowski, Sandra, Hofmann, Birte, Jambor, Ivan, Lehtiö, Kaisa, Rantala, Tuija, Rottmann, Antje, Sipilä, Henri, Sparks, Rick, Suilamo, Sami, Tolvanen, Tuula, Valencia, Ray, Minn, Heikki
• Format: Journal Article
• Language: English
• Published: New York Society of Nuclear Medicine 01.06.2013
• Subjects: Men; Metabolism; Metabolites; Pharmacology; Radiation
• ISSN: 0161-5505; 1535-5667

This first-in-human study investigated the safety, tolerability, metabolism, pharmacokinetics, biodistribution, and radiation dosimetry of ...-bombesin antagonist ...-DOTA-4-amino-1-carboxymethylpiperidine-d-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH... (BAY 86-7548). 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. 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. 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. (ProQuest: ... denotes formulae/symbols omitted.)