Drug intelligence / Profile preview

lesinurad + metformin

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

Overview

Lesinurad + metformin is a combination of two small molecule drugs, lesinurad and metformin. Lesinurad is a selective uric acid reabsorption inhibitor (URAT1 and OAT4 inhibitor) mainly used in the management of hyperuricemia associated with gout, in combination with a xanthine oxidase inhibitor. Metformin is a biguanide oral antihyperglycemic agent widely used for the treatment of type 2 diabetes. There is no approved fixed-dose or branded combination product of lesinurad with metformin; however, both drugs have been studied together in pharmacokinetic interaction trials. These studies demonstrated that oral co-administration of lesinurad (400 mg) with metformin (850 mg) does not result in a clinically significant drug-drug interaction or alter the plasma exposure of metformin. Each drug retains its independent mechanism of action: lesinurad increases renal uric acid excretion by inhibiting URAT1 and OAT4 transporters, while metformin lowers hepatic glucose production and improves insulin sensitivity[1][2][3][4].

02

Targets

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

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