Rolofylline (KW-3902) is an experimental
diuretic
A diuretic () is any substance that promotes diuresis, the increased production of urine. This includes forced diuresis. A diuretic tablet is sometimes colloquially called a water tablet. There are several categories of diuretics. All diuretics in ...
which acts as a selective
adenosine A1 receptor
The adenosine A1 receptor is one member of the adenosine receptor group of G protein-coupled receptors with adenosine as endogenous ligand.
Biochemistry
A1 receptors are implicated in sleep promotion by inhibiting wake-promoting cholinergic neu ...
antagonist.
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
Clinical trials are prospective biomedical or behavioral research studies on human subject research, human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel v ...
(PROTECT) showed the drug to be no better than
placebo
A placebo ( ) is a substance or treatment which is designed to have no therapeutic value. Common placebos include inert tablets (like sugar pills), inert injections (like Saline (medicine), saline), sham surgery, and other procedures.
In general ...
for patients with acute heart failure. Participants given rolofylline did show some improvement in
shortness of breath
Shortness of breath (SOB), also medically known as dyspnea (in AmE) or dyspnoea (in BrE), is an uncomfortable feeling of not being able to breathe well enough. The American Thoracic Society defines it as "a subjective experience of breathing di ...
, 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
seizure
An epileptic seizure, informally known as a seizure, is a period of symptoms due to abnormally excessive or synchronous neuronal activity in the brain. Outward effects vary from uncontrolled shaking movements involving much of the body with l ...
s and
stroke.
References
Adenosine receptor antagonists
Diuretics
Xanthines
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