Drug intelligence / Profile preview

Dimethyl Fumarate + Montelukast

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

Overview

The combination of dimethyl fumarate (DMF) and montelukast is primarily utilized to mitigate gastrointestinal (GI) side effects associated with dimethyl fumarate treatment in patients with multiple sclerosis (MS). Dimethyl fumarate (Tecfidera) is an immunomodulator approved for treating relapsing forms of MS, but its GI side effects frequently challenge therapy adherence, potentially leading to delayed titration or discontinuation. Montelukast (Singulair), a leukotriene receptor antagonist primarily indicated for asthma, exercise-induced bronchoconstriction, and allergic rhinitis, has been repurposed for this adjunctive role. The proposed mechanism involves montelukast's effect on eosinophils, which may contribute to Tecfidera-related GI issues. This approach has been explored in studies, including the MITIGATE trial, to formally assess montelukast's role in improving dimethyl fumarate tolerability. Additionally, a 2024 retrospective study suggested that montelukast may offer an independent benefit in MS patients by significantly reducing relapse rates.

02

Targets

RELA (Nuclear Factor Kappa B Subunit p65)CYSLTR1 (Cysteinyl-leukotriene type 1 receptor)KEAP1 (Kelch-like ECH-associated protein 1)

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