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Initial Clinical Experience With Regadenoson, a Novel Selective A_2A Agonist for Pharmacologic Stress Single-Photon Emission Computed Tomography Myocardial Perfusion Imaging

Robert C. Hendel, MD^_*,1,2,_*, Timothy M. Bateman, MD^1,2,, Manuel D. Cerqueira, MD^1,2,, Ami E. Iskandrian, MD^1,, Jeffrey A. Leppo, MD^1,||, Brent Blackburn, PhD^¶ and John J. Mahmarian, MD^1,2,#

^_* Rush University Medical Center, Chicago, Illinois
Cardiovascular Consultants, Kansas City, Missouri
Cleveland Clinic, Cleveland, Ohio
University of Alabama at Birmingham, Birmingham, Alabama
^|| Berkshire Medical Center, Pittsfield, Massachusetts
^¶ CV Therapeutics, Palo Alto, California
^# Methodist DeBakey Heart Center, The Methodist Hospital/Baylor College of Medicine, Houston, Texas

View larger version (10K): [in a new window]   Figure 1 The molecular structure of regadenoson (CVT-3146; (1-{9-[(4S, 2R, 3R, 5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2yl]-6aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide).

View larger version (16K): [in a new window]   Figure 2 Change in heart rate in beats/min (A) and in systolic blood pressure in mm Hg (B) from baseline after regadenoson administration; values are means with standard errors. Open squares = 400 µg; solid squares = 500 µg.

View larger version (141K): [in a new window]   Figure 3 Direct comparison of adenosine and regadenoson images using a dual-isotope protocol (rest: thallium-201, stress: Tc-99m tetrofosmin). These images reveal a large, mild, reversible perfusion defect in the anterior, apical, and lateral walls. Similar findings were noted on the adenosine and regadenoson stress images. Upper panel is the regadenoson study.