Drug intelligence / Profile preview

Tranilast + allopurinol

Development stage
Discontinued
Lead developer
Nuon Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

Tranilast + allopurinol is a fixed-dose oral combination of two small molecule drugs developed for the treatment of gout and hyperuricemia. Tranilast is an anthranilic acid derivative with uricosuric and anti-inflammatory properties, acting primarily by inhibiting major reabsorptive urate transporters such as SLC22A12 protein (URAT1), SLC2A9 protein (GLUT9), OAT4, and OAT10, leading to increased excretion of uric acid[4]. It also has immunomodulatory effects and can inhibit the NLRP3 inflammasome[5]. Allopurinol is a purine analog that acts as a xanthine oxidase inhibitor to reduce the production of uric acid in the body[6][8]. The combination was intended to provide dual mechanisms for lowering serum urate levels—by both reducing production (allopurinol) and increasing excretion (tranilast). The product was developed by Nuon Therapeutics under the code name NU-1618 but development was discontinued after phase 2 trials for gout and hyperuricemia[2].

Brand names
Combination 400Combination400Combination-400
Other names
tranilast/allopurinol
02

Targets

OAT4 (Solute carrier family 22 member 11)OAT10 (Solute carrier family 22 member 13)URAT1 (Uric Acid Transporter 1)SMCT1 (Sodium-coupled monocarboxylate transporter 1)XO (Xanthine Oxidoreductase)GLUT9 (Glucose transporter type 9)NLRP3 (Nod-like receptor family pyrin domain-containing protein 3)

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