Drug intelligence / Profile preview

lesinurad + furosemide

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

**lesinurad + furosemide** is a combination of two small-molecule drugs: - **Lesinurad** is a selective uric acid reabsorption inhibitor, primarily indicated for use in combination with xanthine oxidase inhibitors for the treatment of hyperuricemia associated with gout. It acts by selectively inhibiting renal urate transporter 1 (URAT1) and organic anion transporter 4 (OAT4), which results in increased uric acid excretion and a reduction in serum uric acid levels. Lesinurad is metabolized mainly through CYP2C9 and is highly protein bound[2][3][4][6]. - **Furosemide** is a loop diuretic indicated for the treatment of edema associated with congestive heart failure, liver cirrhosis, and renal disease, as well as for hypertension. Its principal mechanism involves inhibiting the sodium-potassium-chloride cotransporter (NKCC2) in the thick ascending limb of the loop of Henle, resulting in increased excretion of sodium, chloride, water, and other electrolytes via the urine[5]. In controlled studies, co-administration of lesinurad and furosemide led to a decrease in furosemide plasma exposure (Cmax and AUC), with no clinically significant impact on the diuretic efficacy of furosemide[1]. The effect is likely due to decreased gastrointestinal absorption of furosemide when taken together with lesinurad[1]. There is currently no marketed fixed-dose combination product containing both lesinurad and furosemide, and this combination is not a standard therapy.

02

Targets

OATP1B1 (Organic anion transporting polypeptide 1B1)OAT1 (Organic anion transporter 1)URAT1 (Uric Acid Transporter 1)SLC22A8 (Organic anion transporter 3)GLUT9 (Glucose transporter type 9)OCT1 (Organic cation transporter 1)OAT4 (Solute carrier family 22 member 11)

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