Drug intelligence / Profile preview

lesinurad + calcium carbonate

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

Overview

This is a non-standard, experimental drug combination consisting of **lesinurad**, a selective uric acid reabsorption inhibitor (URAT1 inhibitor) used to lower serum uric acid in patients with gout, and **calcium carbonate**, a commonly used antacid and calcium supplement. No branded or combination product containing both drugs as fixed ingredients is approved. Lesinurad increases urinary excretion of uric acid by inhibiting URAT1 in the kidney. Calcium carbonate works by neutralizing gastric acid and supplying elemental calcium. When co-administered, especially at high calcium carbonate doses, calcium carbonate may decrease the absorption and efficacy of lesinurad, leading to lower plasma concentration and reduced uric acid-lowering effect, likely via ion complexation and changes in gastrointestinal pH. There is no evidence this combination is used therapeutically as a fixed combination, but it has been tested in pharmacokinetic interaction studies to characterize potential reduction in lesinurad efficacy due to co-administration with common antacids[1][3]. Calcium carbonate does not have urate-lowering properties and is not itself a treatment for gout; rather, it is sometimes co-administered as an antacid in patients on multiple medications[8][1].

02

Targets

URAT1 (Uric Acid Transporter 1)OAT4 (Solute carrier family 22 member 11)

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