Drug intelligence / Profile preview

rolofylline + furosemide

Development stage
Phase 2
Lead developer
Merck
Modality
Small Molecules
Administration
Intravenous, Oral (for Furosemide), Possibly Intramuscular (for Furosemide)
01

Overview

**Rolofylline + furosemide** is a combination of an adenosine A1 receptor antagonist (rolofylline) and a potent loop diuretic (furosemide) investigated for the treatment of acute decompensated heart failure (ADHF) with volume overload, especially in patients with renal impairment or diuretic resistance. - **Rolofylline** blocks the adenosine A1 receptor, enhancing diuresis and natriuresis by reducing sodium reabsorption in the renal proximal tubule and mitigating the compensatory renal vasoconstriction and sodium retention mechanisms triggered by loop diuretics, potentially preventing the decline in glomerular filtration rate and preserving renal function[1][4][5]. - **Furosemide** inhibits the sodium-potassium-chloride cotransporter (NKCC2) in the thick ascending limb of the loop of Henle, increasing excretion of sodium, potassium, chloride, and water, leading to diuresis[2]. This combination is studied to augment diuretic response, improve congestion, and support renal function in heart failure.

02

Targets

ADORA1 (Adenosine receptor A1 subtype)NKCC2 (Sodium-potassium-chloride cotransporter 2)

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