Key result
Rolofylline, an adenosine A1-receptor antagonist, advances to Phase III trials for acute heart failure.
Why the study?
Early phase clinical research data provided proof-of-concept for rolofylline's incremental effect beyond standard diuretic therapy in acute heart failure.
Rolofylline is an adenosine A1-receptor antagonist that enhances natriuresis and diuresis, with ongoing Phase III trials for the treatment of acute heart failure.
Rolofylline confers no benefit on the primary composite endpoint in acute HF with renal dysfunction; challenges early-phase promise and ends further development.
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.
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Chaparro et al. (2008) conducted a review in Acute Congestive Heart Failure. Rolofylline (KW-3902) was evaluated. Rolofylline is an adenosine A1-receptor antagonist currently undergoing Phase III clinical trials for the treatment of acute heart failure.
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