RT Journal Article SR Electronic T1 Plasma Pharmacokinetics, Whole-Body Distribution, Metabolism, and Radiation Dosimetry of 68Ga Bombesin Antagonist BAY 86-7548 in Healthy Men JF Journal of Nuclear Medicine JO J Nucl Med FD Society of Nuclear Medicine SP 867 OP 872 DO 10.2967/jnumed.112.114082 VO 54 IS 6 A1 Anne Roivainen A1 Esa Kähkönen A1 Pauliina Luoto A1 Sandra Borkowski A1 Birte Hofmann A1 Ivan Jambor A1 Kaisa Lehtiö A1 Tuija Rantala A1 Antje Rottmann A1 Henri Sipilä A1 Rick Sparks A1 Sami Suilamo A1 Tuula Tolvanen A1 Ray Valencia A1 Heikki Minn YR 2013 UL http://jnm.snmjournals.org/content/54/6/867.abstract AB This first-in-human study investigated the safety, tolerability, metabolism, pharmacokinetics, biodistribution, and radiation dosimetry of 68Ga-bombesin antagonist 68Ga-DOTA-4-amino-1-carboxymethylpiperidine-d-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2 (BAY 86-7548). 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. 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. 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.