PT  - JOURNAL ARTICLE
AU  - Roivainen, Anne
AU  - Kähkönen, Esa
AU  - Luoto, Pauliina
AU  - Borkowski, Sandra
AU  - Hofmann, Birte
AU  - Jambor, Ivan
AU  - Lehtiö, Kaisa
AU  - Rantala, Tuija
AU  - Rottmann, Antje
AU  - Sipilä, Henri
AU  - Sparks, Rick
AU  - Suilamo, Sami
AU  - Tolvanen, Tuula
AU  - Valencia, Ray
AU  - Minn, Heikki
TI  - Plasma Pharmacokinetics, Whole-Body Distribution, Metabolism, and Radiation Dosimetry of <sup>68</sup>Ga Bombesin Antagonist BAY 86-7548 in Healthy Men
AID  - 10.2967/jnumed.112.114082
DP  - 2013 Jun 01
TA  - Journal of Nuclear Medicine
PG  - 867--872
VI  - 54
IP  - 6
4099  - http://jnm.snmjournals.org/content/54/6/867.short
4100  - http://jnm.snmjournals.org/content/54/6/867.full
SO  - J Nucl Med2013 Jun 01; 54
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.