Rolofylline

DB12670InvestigationalSmall molecule

Rolofylline is under clinical development by pharmaceutical company NovaCardia for the treatment of congestive heart failure.

Mechanism: Rolofylline is an adenosine A1-receptor antagonist. Plasma adenosine levels are elevated in patients with heart failure and adenosine A1 receptors in the kidney mediate vasoconstriction of afferent arterioles, reabsorption of sodium and water in proximal tubules, and tubuloglomerular feedback in the juxtaglomerular apparatus. Accordingly, inhibition of these receptors would be expected to increase renal blood flow and enhance diuresis. The effects of Rolofylline on renal function are consistent with those obtained with another adenosine A1-receptor antagonist in both experimental and human heart failure.
Curator reviewed
Formula / weight: C₂₀H₂₈N₄O₂ · 356.47 g/mol (avg)
Code names: KW-3902 · MK-7418

Resolves to

Compound

Structure

InChIKeyPJBFVWGQFLYWCB-QUYAXPHCSA-NSMILESCCCN1C2=C(NC(=N2)C23C[C@@H]4CC2C[C@H](C3)C4)C(=O)N(CCC)C1=O

Targets

What you can answer from here — as of June 15, 2026

1Protein targetEach mapped to UniProt, with action and pharmacological action

Listed above

640Drug interactionsStructured to mechanism, not free text

3Clinical trialsPhase, status and sponsor resolved per trial

4+ReferencesStructured and connected to the statements they support

Which drugs share a target with Rolofylline, and which of those have an active Phase 3 trial?

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