Biodistribution, Safety Profile, and Radiation Dosimetry of [ 18 F]SYN2, a PET Cardiac Perfusion Tracer, in Healthy Subjects

• Published in: Journal of Nuclear Medicine Vol. 66; no. 4; pp. 626 - 633
• Main Authors: Knuuti, Juhani, Kobylecka, Małgorzata, Krajewski, Seweryn, Steczek, Lukasz, Gotowicz, Karina, Towpik, Joanna, Kalliokoski, Kari, Tolvanen, Tuula, Kostkiewicz, Magdalena, Kozanecki, Przemysław, Włostowska, Joanna, Dziuk, Mirosław, Królicki, Leszek, Bil, Jacek, Slomka, Piotr J., Bateman, Timothy M., Al-Mallah, Mouaz H., Chareonthaitawee, Panithaya, Soman, Prem, Kozanecki, Cezary
• Format: Journal Article
• Language: English
• Published: United States 01.04.2025
• Subjects: Adult; Female; Fluorine Radioisotopes; Healthy Volunteers; Heart - diagnostic imaging; Humans; Male; Middle Aged; Myocardial Perfusion Imaging - methods; Positron-Emission Tomography - methods; Radiometry; Radiopharmaceuticals - adverse effects; Radiopharmaceuticals - pharmacokinetics; Safety; Tissue Distribution; [18F]tracer; [18F]SYN2; PET imaging; phase I clinical study; MPI; cardiac imaging
• ISSN: 0161-5505; 2159-662X; 1535-5667
• DOI: 10.2967/jnumed.124.268872

A first-in-human phase I clinical study aimed to assess the safety profile, radiation dosimetry, and biodistribution of a potential cardiac PET myocardial perfusion imaging tracer, [ F]SYN2 ( F-labeled acridine derivative), in healthy subjects. [ F]SYN2 intravenous administration with PET imaging was performed on healthy volunteers, and sequential whole-body imaging was performed over 4 h. Blood and urine samples were collected for up to 240 min. Safety follow-up visits took place at 2, 5, and 14 d after the administration. Ten subjects (8 women and 2 men) completed all study procedures. The mean age was 38.1 ± 8.8 y, and the mean body mass index was 22.7 ± 3.0 kg/m The mean administered dose of radioactivity was 258 MBq (range, 246-272 MBq). There were no drug-related adverse events, and the tracer was well tolerated in all subjects. The mean whole-body effective radiation dose for [ F]SYN2 was 0.0195 mSv/MBq. The tracer was rapidly taken up by the myocardial wall and cleared from plasma, leading to good image quality within minutes of tracer injection. On the basis of the safety profile, radiation dosimetry, and biodistribution of [ F]SYN2, it appears to be a promising agent for clinical PET myocardial perfusion imaging and to warrant further clinical studies.