Rolofylline Explained

Rolofylline (KW-3902) is an experimental diuretic which acts as a selective adenosine A1 receptor antagonist.^{[1] [2]} It was discovered at NovaCardia, Inc. which was purchased by Merck & Co., Inc. in 2007.

Development of rolofylline was terminated on September 1, 2009, after the results of a large clinical trial (PROTECT) showed the drug to be no better than placebo for patients with acute heart failure. Participants given rolofylline did show some improvement in shortness of breath, but the drug did not prevent kidney damage or have any significant effect on overall treatment success. Rolofylline was also associated with a higher incidence of seizures and stroke.^[3]

Notes and References

1. Givertz MM, Massie BM, Fields TK, Pearson LL, Dittrich HC . The effects of KW-3902, an adenosine A1-receptor antagonist, on diuresis and renal function in patients with acute decompensated heart failure and renal impairment or diuretic resistance . J. Am. Coll. Cardiol. . 50 . 16 . 1551–60 . October 2007 . 17936154 . 10.1016/j.jacc.2007.07.019 .
2. Cotter G, Dittrich HC, Weatherley BD, Bloomfield DM, O'Connor CM, Metra M, Massie BM . The PROTECT pilot study: a randomized, placebo-controlled, dose-finding study of the adenosine A1 receptor antagonist rolofylline in patients with acute heart failure and renal impairment . Journal of Cardiac Failure . 14 . 8 . 631–40 . October 2008 . 18926433 . 10.1016/j.cardfail.2008.08.010 .
3. News: Rolofylline fails to PROTECT in acute heart failure . Hughes . Sue . September 1, 2009 . . 2009-09-02.