Dosimetry, biodistribution, and safety of flurpiridaz F 18 in healthy subjects undergoing rest and exercise or pharmacological stress PET myocardial perfusion imaging

• Published in: Journal of nuclear cardiology Vol. 26; no. 6; pp. 2018 - 2030
• Main Authors: Maddahi, Jamshid, Bengel, Frank, Czernin, Johannes, Crane, Paul, Dahlbom, Magnus, Schelbert, Heinrich, Sparks, Richard, Phelps, Michael, Lazewatsky, Joel
• Format: Journal Article
• Language: English
• Published: Cham Elsevier Inc 01.12.2019; Springer International Publishing; Springer Nature B.V
• Subjects: Adenosine; Adenosine - pharmacology; Adult; Cardiology; Dosimetry; dosimetry and biodistribution; Electrocardiography; Exercise; exercise cardiac PET imaging; Exercise Test; Female; Flurpiridaz; Healthy Volunteers; Humans; Imaging; Male; Medicine; Medicine & Public Health; Myocardial Perfusion Imaging; myocardial perfusion PET imaging; Nuclear Medicine; Original Article; Patient Safety; Positron-Emission Tomography; Pyridazines - pharmacokinetics; Radiology; Radiometry - methods; Radiopharmaceuticals - pharmacokinetics; safety; Tomography; Whole Body Imaging; Young Adult; DE; myocardial perfusion PET imaging; AE; Flurpiridaz; dosimetry and biodistribution; EEG; MPI; ECG; ROI; mSv; SD; mCi; safety; rem; ID; MBq; PET; exercise cardiac PET imaging; BMI; ED
• ISSN: 1071-3581; 1532-6551; 1532-6551
• DOI: 10.1007/s12350-018-01484-z

The objectives of this study were to evaluate radiation dosimetry, biodistribution, human safety, and tolerability of 18F-labeled flurpiridaz (Flurpiridaz) in normal subjects undergoing rest and separate-day exercise or adenosine pharmacological stress PET imaging. 12 normal subjects were injected with 58.5 to 121 MBq (1.58 to 3.27 mCi) of Flurpiridaz intravenously at rest on Day 1 and 57 to 171 MBq (1.54 to 4.61 mCi) during stress on Day 2. Sequential whole-body imaging was performed for 5 hours. Blood samples were collected for up to 8 hours. The heart wall received the largest mean absorbed dose with both exercise and adenosine stresses. The mean effective dose was 0.054 rem/mCi (0.015 mSv/MBq) with exercise and 0.069 rem/mCi (0.019 mSv/MBq) with adenosine pharmacological stress. The maximum dose that may be administered without exceeding 1 rem (10 mSv) effective dose was 19 mCi (685 MBq) for exercise and 15 mCi (539 MBq) for adenosine pharmacological stress. There were no drug-related adverse events, and the tracer was well tolerated in all subjects. Based on radiation dosimetry, biodistribution, and safety observations, 18F-labeled flurpiridaz is found suitable for clinical PET myocardial perfusion imaging in conjunction with either exercise or pharmacological stress testing.