Evaluation of the Novel Myocardial Perfusion Positron-Emission Tomography Tracer 18 F-BMS-747158-02

Abstract

Background— Positron-emission tomography (PET) tracers for myocardial perfusion are commonly labeled with short-lived isotopes that limit their widespread clinical use. 18 F-BMS-747158-02 ( 18 F-BMS) is a novel pyridaben derivative that was evaluated for assessment of myocardial perfusion by comparison with 13 N-ammonia ( 13 NH 3 ) and with radioactive microspheres in a pig model. Methods and Results— Fourteen pigs injected with 500 MBq of 13 NH 3 or 100 to 200 MBq of 18 F-BMS underwent dynamic PET at rest and during pharmacological stress. In 8 of these pigs, 18 F-BMS was injected during stress combined with transient, 2.5-minute constriction of the left anterior descending coronary artery. Radioactive microspheres were coinjected with 18 F-BMS. Ratios of myocardial tracer uptake to surrounding tissues were determined, and myocardial blood flow was quantified by compartmental modeling. Both tracers showed high and homogeneous myocardial uptake. Compared with 13 NH 3 , 18 F-BMS showed higher activity ratios between myocardium and blood (rest 2.5 versus 4.1; stress 2.1 versus 5.8), liver (rest 1.2 versus 1.8; stress 0.7 versus 2.0), and lungs (rest 2.5 versus 4.2; stress 2.9 versus 6.4). Regional myocardial blood flow assessed with 18 F-BMS PET showed good correlation ( r =0.88, slope=0.84) and agreement (mean difference −0.10 [25th percentile −0.3, 75th percentile 0.1 mL · min −1 · g −1 ]) with that measured with radioactive microspheres over a flow range from 0.1 to 3.0 mL · min −1 · g −1 . The extent of defects induced by left anterior descending coronary artery constriction measured by 18 F-BMS and microspheres also correlated closely ( r =0.63, slope=1.1). Conclusions— 18 F-BMS-747158-02 is a very attractive new PET perfusion tracer that allows quantitative assessment of regional myocardial perfusion over a wide flow range. The long half-life of 18 F renders this tracer useful for clinical PET/CT applications in the workup of patients with suspected or proven coronary artery disease.