Drug intelligence / Profile preview

dimethyl fumarate + acetylsalicylic acid

Development stage
Phase 4
Lead developer
Biogen
Modality
Small Molecules
Administration
Oral
01

Overview

**dimethyl fumarate + acetylsalicylic acid** is a combination of two small molecules: dimethyl fumarate, an approved oral immunomodulator for relapsing forms of multiple sclerosis, and acetylsalicylic acid (aspirin), a cyclooxygenase inhibitor. This combination is not a branded or marketed fixed-dose product but refers to the clinical co-administration of these agents. The rationale for co-administration is to mitigate dimethyl fumarate–induced flushing, a prostaglandin-mediated side effect, by giving acetylsalicylic acid before dimethyl fumarate dosing. There is clinical evidence that pretreatment with 325 mg acetylsalicylic acid reduces the incidence and severity of flushing associated with dimethyl fumarate without affecting its pharmacokinetic profile or efficacy. Dimethyl fumarate acts via anti-inflammatory and cytoprotective mechanisms, likely involving the nuclear factor (erythroid-derived 2)-like 2 (Nrf2) antioxidant response pathway and inhibition of proinflammatory cytokines. Acetylsalicylic acid irreversibly inhibits cyclooxygenase enzymes, reducing the synthesis of prostaglandins implicated in the flushing reaction and mediating antiplatelet, analgesic, antipyretic, and anti-inflammatory activities[1][3][4][5].

Other names
dimethyl fumarate and acetylsalicylic acidDMF + ASAdimethyl fumarate + aspirin
02

Targets

PGHS-1 (Prostaglandin G/H Synthase 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)KEAP1 (Kelch-like ECH-associated protein 1)NFE2L2 (Nuclear factor (erythroid-derived 2)-like 2)

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