Structure via PubChem · Public domain (PubChem)
rolofylline
Sign in to saveAlso known as KW-3902, NAX
Rolofylline (KW-3902) is an experimental diuretic which acts as a selective adenosine A1 receptor antagonist. It was discovered at NovaCardia, Inc. which was purchased by Merck & Co., Inc. in 2007.
Chemical data
- Formula
- C20H28N4O2
- Molecular weight
- 356.5 g/mol
- IUPAC name
- 1,3-dipropyl-8-(3-tricyclo[3.3.1.03,7]nonanyl)-7H-purine-2,6-dione
via PubChem
Drug data · ChEMBL
- Max clinical phase
- Phase 3
- Molecule type
- Small molecule
- Indications
- heart failure, congestive heart failure
via ChEMBL · EBI
Research
122 papers- Rolofylline: a selective adenosine 1 receptor antagonist for the treatment of heart failure.Expert opinion on pharmacotherapy · 2009
- Rolofylline, an adenosine A1-receptor antagonist, in acute heart failure.The New England journal of medicine · 2010
- Rolofylline, an adenosine A1 receptor antagonist, inhibits osteoclast differentiation as an inverse agonist.British journal of pharmacology · 2013
- Simultaneous pharmacokinetic model for rolofylline and both M1-trans and M1-cis metabolites.The AAPS journal · 2013
- Adenosine A1 receptor antagonist rolofylline alleviates axonopathy caused by human Tau ΔK280.Proceedings of the National Academy of Sciences of the United States of America · 2016
via PubMed
Wikidata facts
- Mass
- 356.221226
Show 2 more facts
- chemical formula
- C₂₀H₂₈N₄O₂
- canonical SMILES
- CCCN1C2=C(C(=O)N(C1=O)CCC)NC(=N2)C34CC5CC(C3)CC4C5
Sources (2)
via Wikidata · CC0
~1 min read
Article
1 sectionsContents
- References
Rolofylline (KW-3902) is an experimental diuretic which acts as a selective adenosine A1 receptor 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 (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.
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