Drug intelligence / Profile preview

Tranilast + febuxostat

Development stage
Phase 2
Lead developer
Teijin Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

Tranilast + febuxostat is a combination of two small molecule drugs investigated for the treatment of hyperuricemia and gout. Febuxostat is a xanthine oxidase inhibitor that reduces uric acid production by non-competitively inhibiting the molybdenum pterin center of xanthine oxidase, thereby lowering serum urate levels[1][6]. Tranilast acts as a potent uricosuric agent by inhibiting major reabsorptive urate transporters in the kidney, including Urate transporter 1 (URAT1), Glucose transporter 9 (GLUT9), Organic anion transporter 4 (OAT4), and Organic anion transporter 10 (OAT10). This results in increased excretion of uric acid in urine[4]. The combination has been studied in phase 2 clinical trials for its potential to more effectively manage hyperuricemia and prevent gout flares compared to monotherapy[2].

02

Targets

GLUT9 (Glucose transporter type 9)OAT10 (Solute carrier family 22 member 13)OAT4 (Solute carrier family 22 member 11)URAT1 (Uric Acid Transporter 1)XO (Xanthine Oxidoreductase)

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