Phase I, First-in-Human Study of BMS747158, a Novel 18F-Labeled Tracer for Myocardial Perfusion PET: Dosimetry, Biodistribution, Safety, and Imaging Characteristics After a Single Injection at Rest

• DOI: 10.2967/jnumed.111.092528
• Publication Date: 2011-08-18T00:55:47Z
• Authors: Jamshid Maddahi; Johannes Czernin; Joel Lazewatsky; Sung-Cheng Huang; Magnus Dahlbom; Heinrich Schelbert; Richard Sparks; Alexander Ehlgen; Paul Crane; Qi Zhu; Marybeth Devine; Michael Phelps
• Keywords: Biodistribution

¹⁸F-labeled BMS747158 is a novel myocardial perfusion imaging tracer that targets mitochondrial complex 1. The objectives of this phase I study were to evaluate radiation dosimetry, biodistribution, human safety, tolerability, and early elimination ¹⁸F activity in urine after injection single dose the at rest healthy subjects. <b>Methods:</b> Thirteen subjects injected with 170–244 MBq (4.6–6.6 mCi) intravenously. Dynamic PET was obtained over heart for 10 min, followed by sequential whole-body 5 h. Blood samples urinary excretion collected up 8 Heart rate, electrocardiogram, blood pressure monitored before during imaging. residence times determined from multiexponential regression organ region-of-interest data normalized dose. Absorbed estimates all target organs using MIRD schema OLINDA/EXM software. <b>Results:</b> receiving largest mean absorbed kidneys 0.066 mSv/MBq (0.24 rem/mCi), wall 0.048 (0.18 rem/mCi). effective 0.019 (0.072 exhibited high sustained retention earliest images through approximately h injection. There no drug-related adverse events, well tolerated Mean 4.83 percentage (range, 0.64–12.41 dose). <b>Conclusion:</b> These preliminary suggest appears be has unique potential PET.