Initial Clinical Experience With Regadenoson, a Novel Selective A2AAgonist for Pharmacologic Stress Single-Photon Emission Computed Tomography Myocardial Perfusion Imaging
Open accessAbstract
Objectives Regadenoson, a selective A2A adenosine receptor agonist, was evaluated for tolerability and effectiveness as a pharmacological stress agent for detecting reversible myocardial hypoperfusion when combined with single-photon emission computed tomography (SPECT).Background Adenosine and dipyridamole are nonselective adenosine agonists currently used as pharmacologic stressors. Despite proven safety, these agents often cause undesirable side effects and require a continuous infusion.Methods This Phase II, multicenter, open-label trial was conducted in 36 patients who had demonstrated ischemia on a 6-min adenosine SPECT imaging study within the previous 2 to 46 days. Patients received regadenoson as a rapid intravenous bolus dose of 400 microg (n = 18) or 500 microg (n = 18). The radiopharmaceutical was then delivered within one minute. The SPECT images were acquired in a standard manner and uniformly processed at a central laboratory. Regadenoson and adenosine studies were presented in random order and interpreted blindly with a 17-segment model by three observers. Additionally, quantitative analysis was performed with 4D-MSPECT software (University of Michigan, Ann Arbor, Michigan).Results Overall agreement for the presence of reversible hypoperfusion was 86%. The 400-mug dose was better tolerated. Overall, regadenoson was well-tolerated; side effects (e.g., chest discomfort, flushing, dyspnea) were generally mild in severity and self-limiting. High-grade atrioventricular block and bronchospasm were not observed.Conclusions Regadenoson is well-tolerated and seems as effective as adenosine for detecting and quantifying the extent of hypoperfusion observed with SPECT perfusion imaging. Phase III clinical trials are now underway, given the promise of regadenoson's reduced side effects and simplicity of bolus administration.
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Regadenoson is a selective A2A adenosine receptor agonist under investigation as a pharmacologic vasodilator in nuclear stress myocardial perfusion imaging (MPI).
“Regadenoson is a selective A 2A adenosine receptor agonist under investigation as a pharmacologic vasodilator in nuclear stress myocardial perfusion imaging (MPI) (1).”
From Interaction of Caffeine With Regadenoson-Induced Hyperemic Myocardial Blood Flow as Measured by Positron Emission Tomography (2008) · cites this paper as [1]
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- Authors
- Hendel, R. C., Bateman, T. M., Cerqueira, M. D., Iskandrian, A. E., Leppo, J. A., Blackburn, B., & Mahmarian, J. J.
- Affiliations
- Rush University Medical Center (US)
- Cleveland Clinic (US)
- University of Alabama at Birmingham (US)
- Berkshire Medical Center (US)
- Houston Methodist (US)
- Corresponding author
- Hendel, Robert C.
- Venue
- Journal of the American College of Cardiology
- Publisher
- Elsevier BV
- Published
- 2005-12
- Volume
- 46
- Issue
- 11
- Pages
- 2069-2075
- ISSN
- 0735-1097 (ISSN-L)
- OpenAlex
- W1984550508
- Cited by
- 128
- References
- 17
- Citations by year
- 2026: 2 · 2025: 3 · 2024: 3 · 2022: 5 · 2021: 5 · 2020: 4 · 2019: 3 · 2018: 4 · 2017: 6 · 2016: 8 · 2015: 10 · 2014: 4 · 2013: 9 · 2012: 12
- FWCI
- 6.13
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Licence
- Locations
- Journal of the American College of Cardiology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Cardiac Imaging and Diagnostics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Physiology › Adenosine and Purinergic Signaling
- Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Medical Imaging Techniques and Applications
- Keywords
- regadenoson, adenosine A2A receptor agonist, pharmacological stress, myocardial perfusion imaging, SPECT, drug tolerability, adverse effects, coronary artery disease
- MeSH terms
- Adenosine, Electrocardiography, Heart, Humans, Organophosphorus Compounds, Pilot Projects, Purines, Pyrazoles, Organotechnetium Compounds, Tomography, Emission-Computed, Single-Photon, Myocardial Ischemia, Technetium Tc 99m Sestamibi, Radiopharmaceuticals, Adenosine A2 Receptor Agonists
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