Rolofylline (KW-3902): A new adenosine A1-receptor antagonist for acute congestive heart failure

Sandra Chaparro, Howard C. Dittrich, W. H.Wilson Tang

Research output: Contribution to journalArticlepeer-review

7 Scopus citations


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.

Original languageEnglish (US)
Pages (from-to)117-123
Number of pages7
JournalFuture Cardiology
Issue number2
StatePublished - Mar 1 2008
Externally publishedYes


  • Adenosine A1 receptor antagonist
  • Cardiorenal syndrome
  • Heart failure
  • KW-3902
  • Natriuresis
  • Renal function
  • Rolofylline

ASJC Scopus subject areas

  • Cardiology and Cardiovascular Medicine
  • Molecular Medicine


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