申请人:Astellas Pharma Inc.
公开号:EP3825302A1
公开(公告)日:2021-05-26
[Problem]
Provided is a labeled fatty acid derivative for diagnostic imaging that enables quantification of fatty acid metabolic activity in the heart muscle.
[Means for Solution]
The present inventors have conducted intensive investigations on a method that enables quantification of fatty acid metabolic activity and thus have found that a labeled fatty acid derivative typified by 3-[(5Z)-3-[18F]fluorotetradeca-5-en-1-yl]sulfanyl}propanoic acid or a salt thereof has excellent accumulation to the heart muscle and thus enables imaging of fatty acid metabolic activity by positron emission tomography (PET). Therefore, the labeled fatty acid derivative of the present invention can be used as a radiolabeled tracer for rapid and non-invasive quantification of fatty acid metabolic activity in the heart muscle, diagnostic imaging of heart disease typified by an ischemic heart disease, diagnostic imaging of the therapeutic effect of a therapeutic drug for heart disease, and the like.
问题
本发明提供了一种用于诊断成像的标记脂肪酸衍生物,该衍生物能够量化心肌中的脂肪酸代谢活动。
[解决方法]
本发明人对一种能够量化脂肪酸代谢活动的方法进行了深入研究,从而发现以 3-[(5Z)-3-[18F]氟十四碳-5-烯-1-基]硫基}丙酸或其盐为典型的标记脂肪酸衍生物在心肌中具有极好的蓄积性,因此能够通过正电子发射断层扫描(PET)对脂肪酸代谢活动进行成像。因此,本发明的标记脂肪酸衍生物可用作放射性标记示踪剂,用于快速、无创地量化心肌中的脂肪酸代谢活性,对以缺血性心脏病为典型特征的心脏病进行诊断成像,对心脏病治疗药物的治疗效果进行诊断成像等。