rolofylline

Rolofylline is a selective and potent small molecule antagonist of the adenosine A1 receptor. It is a xanthine derivative developed primarily for the treatment of acute heart failure and cardiorenal syndrome. By blocking adenosine A1 receptors in the kidney—where these receptors mediate vasoconstriction of afferent arterioles and promote sodium/water reabsorption—rolofylline was designed to increase renal blood flow and enhance diuresis. Clinical studies showed that it could facilitate diuresis and preserve renal function in patients with acute decompensated heart failure with renal dysfunction. Despite promising early results in pilot studies (such as PROTECT), larger phase III trials failed to demonstrate significant clinical benefit over placebo; development was discontinued due to lack of efficacy and safety concerns (notably increased risk of seizures)[1][4][5][6][8].

Other names

Rolofylline [USAN]ROLOFYLLINE [INN]rolofyllinum8-(Hexahydro-2,5-methanopentalen-3a(1H)-yl)-3,7-dihydro-1,3-dipropyl-1H-purine-2,6-dione