Rolofylline: a selective adenosine 1 receptor antagonist for the treatment of heart failure.

Co-existent cardiac and renal dysfunction is increasingly recognized as both a predictor and mediator of poor outcomes in patients with advanced heart failure. Novel therapies, including adenosine receptor antagonists, are currently under development for the treatment of 'cardiorenal syndrome'. To review the pathophysiologic rationale for using rolofylline, a selective adenosine 1 receptor antagonist, in patients with cardiorenal syndrome; and to provide a critical overview of safety and efficacy data from clinical studies. We reviewed published data on the pharmacology of rolofylline, and used this to inform a comprehensive summary of preclinical and clinical trials. Cardiac and renal effects, and safety data with a particular reference to seizures, are highlighted. Rolofylline facilitates diuresis and preserves renal function in patients with acute decompensated heart failure and renal dysfunction. Pilot data also suggest beneficial effects on symptoms and short-term outcomes. The risk of seizures may be minimized by excluding high-risk patients.