Dosimetry, biodistribution, and safety of flurpiridaz F 18 in healthy subjects undergoing rest and exercise or pharmacological stress PET myocardial perfusion imaging
Dosimetry, biodistribution, and safety of flurpiridaz F 18 in healthy subjects undergoing rest and exercise or pharmacological stress PET myocardial perfusion imaging
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DOI：
10.1007/s12350-018-01484-z
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发表时间：
2019-12-01
影响因子：
2.4
通讯作者：
Lazewatsky, Joel
中科院分区：
文献类型：
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作者：
Maddahi, Jamshid;Bengel, Frank;Lazewatsky, Joel
本研究的目的是评价F-18标记的氟吡达兹（氟吡达兹）在接受休息和单独一天运动或腺苷药理学负荷PET成像的正常受试者中的辐射剂量测定、生物分布、人体安全性和耐受性。方法12名正常人在第1天安静时静脉注射氟吡达58.5 ~ 121 MBq（1.58 ~ 3.27 mCi），第2天应激时静脉注射氟吡达57 ~ 171 MBq（1.54 ~ 4.61 mCi）。进行连续全身成像5小时。采集血样长达8小时。结果运动负荷和腺苷负荷下，心脏壁所受的平均吸收剂量最大。运动时的平均有效剂量为0.054 rem/mCi（0.015 mSv/MBq），腺苷药理应激时的平均有效剂量为0.069 rem/mCi（0.019 mSv/MBq）。在不超过1 rem（10 mSv）有效剂量的情况下，运动时可给予的最大剂量为19 mCi（685 MBq），腺苷药理学应激时为15 mCi（539 MBq）。没有药物相关的不良事件，示踪剂在所有受试者中耐受良好。结论基于辐射剂量学、生物分布和安全性观察，发现F-18标记的氟吡达适用于临床PET心肌灌注成像结合运动或药理学负荷试验。
The objectives of this study were to evaluate radiation dosimetry, biodistribution, human safety, and tolerability of F-18-labeled flurpiridaz (Flurpiridaz) in normal subjects undergoing rest and separate-day exercise or adenosine pharmacological stress PET imaging. Methods 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. Results 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. Conclusion Based on radiation dosimetry, biodistribution, and safety observations, F-18-labeled flurpiridaz is found suitable for clinical PET myocardial perfusion imaging in conjunction with either exercise or pharmacological stress testing.