Drug intelligence / Profile preview

tegomil fumarate

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

Overview

Riulvy (tegomil fumarate) is an oral disease-modifying therapy developed by the Tiefenbacher Group in collaboration with Neuraxpharm for the treatment of relapsing forms of multiple sclerosis, specifically relapsing-remitting multiple sclerosis (RRMS). As a next-generation fumarate-class small molecule, it acts as a prodrug that is metabolized in the body to monomethyl fumarate (MMF), the active moiety. Tegomil fumarate consists of two MMF molecules linked by a tetraethylene glycol chain, which is cleaved in vivo to release MMF and pharmacologically inactive PEG. Its mechanism of action involves the activation of the Nuclear factor erythroid 2-related factor 2 (NRF2) transcriptional pathway, which exerts anti-inflammatory and cytoprotective effects on the central nervous system. Designed as a hybrid medicine to dimethyl fumarate (Tecfidera), tegomil fumarate aims to provide equivalent efficacy with improved gastrointestinal tolerability by avoiding the production of methanol during metabolism.

Brand names
Riulvy
Other names
Tegomil fumarate
02

Targets

KEAP1 (Kelch-like ECH-associated protein 1)NFE2L2 (Nuclear factor (erythroid-derived 2)-like 2)

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