Tranilast (DB07615): A Comprehensive Pharmacological and Clinical Monograph on a Pleiotropic Immunomodulator

Executive Summary

Tranilast, identified chemically as N-(3,4-Dimethoxycinnamoyl)anthranilic acid, is a small molecule drug with a complex and evolving pharmacological profile. Originally developed by Kissei Pharmaceuticals, it was first approved in Japan and South Korea in 1982 for the management of bronchial asthma, with its indications later expanded to include fibrotic skin conditions such as keloids and hypertrophic scars.[1] For decades, its identity was primarily defined by its anti-allergic properties, rooted in its ability to stabilize mast cell membranes and inhibit the release of inflammatory mediators.[1] This established its long-standing therapeutic role in several Asian countries, including China, where it remains in clinical use for these conditions.[2]

However, subsequent decades of research have unveiled a far more intricate and pleiotropic mechanism of action, fundamentally reshaping its scientific identity from a simple anti-allergic agent to a multifaceted immunomodulator. Beyond mast cell stabilization, Tranilast has been shown to exert potent anti-fibrotic effects through the direct inhibition of the transforming growth factor-beta (TGF-β) signaling pathway, a central mediator of tissue remodeling and fibrosis.[3] More recent discoveries have further expanded its known activities, identifying it as a direct and specific inhibitor of the NLRP3 inflammasome—a key platform in the innate immune system responsible for driving inflammation in a host of metabolic and autoimmune diseases.[5] Additionally, it has been characterized as an inhibitor of the TRPV2 ion channel, implicating it in processes of calcium homeostasis and neuronal function.[7]