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
| العنوان: | 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 |
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| المؤلفون: | Johannes Czernin, Richard B. Sparks, Alexander Ehlgen, Jamshid Maddahi, Joel Lazewatsky, Qi Zhu, Michael E. Phelps, H. Schelbert, Sung-Cheng Huang, Paul D. Crane, Marybeth Devine, Magnus Dahlbom |
| المصدر: | Journal of Nuclear Medicine. 52:1490-1498 |
| بيانات النشر: | Society of Nuclear Medicine, 2011. |
| سنة النشر: | 2011 |
| مصطلحات موضوعية: | Adult, Male, Fluorine Radioisotopes, Biodistribution, Adolescent, Whole-Body Counting, Effective dose (radiation), Young Adult, Myocardial perfusion imaging, Coronary Circulation, Heart rate, Humans, Medicine, Dosimetry, Tissue Distribution, Radiology, Nuclear Medicine and imaging, Radiometry, medicine.diagnostic_test, business.industry, Electroencephalography, Heart, Pyridazines, Positron emission tomography, Positron-Emission Tomography, Absorbed dose, Female, Radiopharmaceuticals, business, Nuclear medicine, Perfusion, Algorithms |
| الوصف: | 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 of 18F activity in urine after injection of a single dose of the tracer at rest in healthy subjects. Methods: Thirteen healthy subjects were injected with 170–244 MBq (4.6–6.6 mCi) of BMS747158 intravenously. Dynamic PET was obtained over the heart for 10 min, followed by sequential whole-body imaging for 5 h. Blood samples and urinary excretion were collected for up to 8 h. Heart rate, electrocardiogram, and blood pressure were monitored before and during imaging. The residence times were determined from multiexponential regression of organ region-of-interest data normalized by injected dose. Absorbed dose estimates for all target organs were determined using MIRD schema with OLINDA/EXM software. Results: The organ receiving the largest mean absorbed dose was the kidneys at 0.066 mSv/MBq (0.24 rem/mCi), followed by the heart wall at 0.048 mSv/MBq (0.18 rem/mCi). The mean effective dose was 0.019 mSv/MBq (0.072 rem/mCi). The heart exhibited high and sustained retention of BMS747158 from the earliest images through approximately 5 h after injection. There were no drug-related adverse events, and the tracer was well tolerated in all subjects. Mean urinary excretion was 4.83 percentage injected dose (range, 0.64–12.41 percentage injected dose). Conclusion: These preliminary data suggest that 18F-labeled BMS747158 appears to be well tolerated and has a unique potential for myocardial perfusion PET. |
| تدمد: | 2159-662X 0161-5505 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d0b9909f016a550ec86296a096da15a9 https://doi.org/10.2967/jnumed.111.092528 |
| حقوق: | OPEN |
| رقم الأكسشن: | edsair.doi.dedup.....d0b9909f016a550ec86296a096da15a9 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 2159662X 01615505 |
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