An Overview of DRF in the treatment of Multiple Sclerosis

Abstract

Diroximel fumarate (DRF) is an oral disease-modifying agent indicated for the treatment of relapsing-remitting multiple sclerosis (RRMS), which is taken twice a day. In EVOLVE-MS-1, Phase 3, a two-year safety study evaluating DRF in patients with RRMS, it is shown that the occurrence of flushing and gastrointestinal treatment-emergent adverse events is comparatively low. This results in a low rate of discontinuation due to treatment-emergent adverse events as compared to dimethyl fumarate (DMF). Monomethyl fumarate (MMF) is a common active metabolite of DMF and DRF. This active metabolite is responsible for the mechanism of actions of the drugs since it crossed the blood-brain barrier. Methanol is the primary metabolite of DMF metabolism but a minor metabolite of DRF metabolism, which results in a lower risk of gastrointestinal symptoms. Both DMF and DRF show similar Tmax and Cmax, which indicate similarity in the efficacy of both the drugs. Therefore, DRF has a similar safety and efficacy profile but better tolerability of treatment-emergent adverse events when compared to DMF. This article provides an updated overview of the pharmacological, therapeutic efficacy, and tolerability of DRF.