Rolofylline (KW-3902): a new adenosine A1-receptor antagonist for acute congestive heart failure.
Rolofylline (KW-3902 or MK-7418) is an adenosine A1-receptor antagonist that exerts its effect by blocking adenosine-mediated constriction of the afferent glomerular arteriole. By blocking A1 receptors, rolofylline increases the glomerular blood flow and filtration and inhibits sodium reabsorption in the proximal tubule, thereby enhancing natriuresis and diuresis. Early phase clinical research data provided the proof-of-concept of an incremental effect beyond standard diuretic therapy. A large Phase III program is currently ongoing for the intravenous formulation of rolofylline in the treatment of acute heart failure.
Cleveland Clinic, Department of Cardiovascular Medicine, 9500 Euclid Avenue, F25, Cleveland, OH 44195, USA. chapars@ccf.org
Sandra
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Chaparro
Howard C
HC
Dittrich
Wh Wilson
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Tang