L-06：Drug Repositioning for Chronic Pain

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＜L-06＞：Life Science, Pharmaceutical Sciences sdgs-03
 

Drug Repositioning for Chronic Pain
― Efficacy of Tranilast in Trigeminal Neuropathic Pain ―

Yoshizo Matsuka Professor
Department of Stomatognathic Function and Occlusal Reconstruction, Clinical Dentistry, Oral Science Graduate School of Biomedical Science
Keywords Neuropathic pain, tetrahydrobiopterin (BH4) metabolic pathway, tranilast
Laboratory URL https://www.2hotetsu-tokushima-u.jp/
Research Overview
● Side Effects of Current Medications Limit Long-Term Treatment for Neuropathic Pain
With the advent of a super-aging society and the nationwide establishment of pain centers, the number of patients suffering from intractable chronic pain, including trigeminal neuropathic pain, is increasing. Trigeminal neuropathic pain is particularly common in elderly patients; however, effective treatment options remain limited, and in many cases, strong drug-related side effects make long-term administration difficult, posing a significant clinical challenge.

● Suppression of the BH4 Metabolic Pathway by an Existing Drug (Tranilast) and Alleviation of Neuropathic Pain
Activation of the tetrahydrobiopterin (BH4) metabolic pathway is associated with chronic pain, and partial inhibition of this pathway has been shown to result in fewer side effects (Fig. 1). In this study, we focused on tranilast, an existing anti-allergic drug known to suppress the BH4 metabolic pathway. Administration of tranilast in a trigeminal neuropathic pain model resulted in significant analgesic effects, demonstrated here for the first time (Figs. 2 and 3).
 
Potential Applications and Commercialization Prospects

● Application of Tranilast to Neuropathic Pain Through Drug Repositioning
Tranilast is an anti-allergic drug reported to affect part of the BH4 metabolic pathway and is currently used clinically for bronchial asthma, keloids, and atopic dermatitis. It is also known to have relatively mild side effects. Because tranilast has already been clinically applied in other indications and has shown efficacy in a trigeminal neuropathic pain model, the regulatory barriers to its approval as a therapeutic agent for neuropathic pain are expected to be relatively low.

L-06-1.png

Fig. 1. BH4 metabolic pathway		 L-06-2.png
Fig. 2. Analgesic effect of tranilast		 L-06-3.png
Fig. 3. Changes in the BH4 pathway induced by tranilast
Publications ● Raman S et al., Analgesic effect of tranilast in an animal model of neuropathic pain and its role in the regulation of tetrahydrobiopterin synthesis. International Journal of Molecular Sciences 23:5878, (2022).

Last updated date：October 15, 2026

 

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