Overview
Dimethyl fumarate is an agent indicated for the treatment of relapsing forms of multiple sclerosis. The mechanism of action of dimethyl fumarate in multiple sclerosis is not well understood. It is thought to involve dimethyl fumarate degradation to its active metabolite monomethyl fumarate (MMF) then MMF up-regulates the Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) pathway that is activated in response to oxidative stress. Dimethyl fumarate is marketed under the brand name Tecfidera, and it was the third oral disease-modifying agent for multiple sclerosis approved by the FDA, following fingolimod and teriflunomide. Prior to its FDA approval, dimethyl fumarate had been used in Germany for treatment of psoriasis.
Indication
Dimethyl fumarate is indicated for the treatment of relapsing forms of multiple sclerosis (MS), including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease, in adults.
Associated Conditions
- Clinically Isolated Syndrome (CIS)
- Relapsing Forms of MS
- Relapsing Remitting Multiple Sclerosis (RRMS)
- Active Secondary Progressive Multiple Sclerosis (SPMS)
Research Report
An Expert Report on Dimethyl Fumarate (DB08908)
Executive Summary
Dimethyl fumarate (DMF) is a pleiotropic oral immunomodulatory agent with established efficacy in the treatment of relapsing forms of multiple sclerosis (MS) and moderate-to-severe plaque psoriasis. Classified as a small molecule, it is the methyl ester of fumaric acid, a compound with historical roots in herbal medicine. Its therapeutic effects are attributed to a complex and multifactorial mechanism of action that is not yet fully elucidated. The primary pathways involve the activation of the Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) antioxidant response pathway, which confers cytoprotective effects against oxidative stress, and the inhibition of the pro-inflammatory Nuclear Factor-kappa B (NF-κB) pathway. This dual action results in a systemic shift from a pro-inflammatory to an anti-inflammatory immune cell phenotype, reducing autoimmune-mediated damage.
In the treatment of MS, marketed as Tecfidera®, pivotal Phase 3 clinical trials (DEFINE and CONFIRM) demonstrated that DMF significantly reduces the annualized relapse rate, delays the progression of physical disability, and markedly decreases MRI lesion activity when compared with placebo. For moderate-to-severe plaque psoriasis, marketed as Skilarence® in the European Union, the pivotal Phase 3 BRIDGE trial established its non-inferiority to a mixed fumaric acid ester formulation and its superiority to placebo in achieving significant skin clearance, as measured by the Psoriasis Area and Severity Index (PASI).
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2025/02/27 | Phase 2 | Recruiting | |||
2024/07/22 | Phase 2 | Recruiting | Pujol, Aurora, M.D. | ||
2023/07/25 | Phase 4 | Not yet recruiting | Beijing Tiantan Hospital | ||
2023/03/14 | N/A | Not yet recruiting | |||
2022/12/20 | Phase 4 | Completed | |||
2022/12/20 | N/A | Recruiting | |||
2022/06/14 | Phase 1 | Active, not recruiting | |||
2021/05/18 | Phase 1 | UNKNOWN | |||
2021/05/18 | Phase 2 | Withdrawn | |||
2021/05/18 | Phase 2 | Withdrawn |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| MSN LABORATORIES PRIVATE LIMITED | 69539-042 | ORAL | 120 mg in 1 1 | 5/13/2021 | |
| TWi Pharmaceuticals, Inc. | 24979-128 | ORAL | 240 mg in 1 1 | 4/25/2022 | |
| Camber Pharmaceuticals, Inc. | 31722-658 | ORAL | 240 mg in 1 1 | 2/19/2024 | |
| Accord Healthcare Inc. | 16729-416 | ORAL | 120 mg in 1 1 | 8/31/2023 | |
| Ascend Laboratories, LLC | 67877-555 | ORAL | 120 mg in 1 1 | 5/19/2023 | |
| Zydus Pharmaceuticals USA Inc. | 70710-1205 | ORAL | 240 mg in 1 1 | 11/9/2022 | |
| Biogen Inc. | 64406-005 | ORAL | 120 mg in 1 1 | 8/19/2022 | |
| Dr. Reddy's Laboratories Inc. | 43598-429 | ORAL | 120 mg in 1 1 | 5/28/2022 | |
| Lupin Pharmaceuticals, Inc. | 68180-777 | ORAL | 240 mg in 1 1 | 12/10/2021 | |
| Ascend Laboratories, LLC | 67877-556 | ORAL | 240 mg in 1 1 | 5/19/2023 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
Authorised | 6/23/2017 | ||
Authorised | 4/22/2024 | ||
Authorised | 4/22/2024 | ||
Authorised | 4/22/2024 |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| TECFIDERA GASTRO-RESISTANT HARD CAPSULES 240 MG | SIN15054P | CAPSULE, ENTERIC COATED | 240.0 mg | 7/26/2016 | |
| TECFIDERA GASTRO-RESISTANT HARD CAPSULES 120 MG | SIN15053P | CAPSULE, ENTERIC COATED | 120.0mg | 7/26/2016 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| No NMPA approvals found for this drug. | |||||
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| TECFIDERA GASTRO-RESISTANT CAPSULES 120MG | N/A | N/A | N/A | 3/29/2016 | |
| TECFIDERA GASTRO-RESISTANT CAPSULES 240MG | N/A | N/A | N/A | 3/29/2016 |
TGA Drug Approvals
Health Canada Drug Approvals
Approved Product | Company | DIN | Dosage Form | Strength | Market Date |
|---|---|---|---|---|---|
| SANDOZ DIMETHYL FUMARATE DELAYED-RELEASE CAPSULES | 02513781 | Capsule (Delayed Release) - Oral | 120 MG | 10/4/2021 | |
| JAMP DIMETHYL FUMARATE | 02516047 | Capsule (Delayed Release) - Oral | 120 MG | 10/4/2021 | |
| SANDOZ DIMETHYL FUMARATE | 02515571 | Capsule (Delayed Release) - Oral | 240 MG | N/A | |
| TECFIDERA | Biogen Canada Inc | 02420201 | Capsule (Delayed Release) - Oral | 240 MG | 2/4/2014 |
| SANDOZ DIMETHYL FUMARATE | 02515563 | Capsule (Delayed Release) - Oral | 120 MG | N/A | |
| MAR-DIMETHYL FUMARATE | marcan pharmaceuticals inc | 02502704 | Capsule (Delayed Release) - Oral | 240 MG | 10/4/2021 |
| JAMP DIMETHYL FUMARATE | 02516055 | Capsule (Delayed Release) - Oral | 240 MG | 10/4/2021 | |
| GLN-DIMETHYL FUMARATE | glenmark pharmaceuticals canada inc. | 02494809 | Capsule (Delayed Release) - Oral | 120 MG | 10/19/2021 |
| GLN-DIMETHYL FUMARATE | glenmark pharmaceuticals canada inc. | 02494817 | Capsule (Delayed Release) - Oral | 240 MG | 10/21/2021 |
| MAR-DIMETHYL FUMARATE | marcan pharmaceuticals inc | 02502690 | Capsule (Delayed Release) - Oral | 120 MG | 10/4/2021 |
CIMA AEMPS Drug Approvals
Approved Product | Company | Registration Number | Pharmaceutical Form | Prescription Type | Status |
|---|---|---|---|---|---|
| No CIMA AEMPS (Spain) approvals found for this drug. | |||||
Philippines FDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Philippines FDA approvals found for this drug. | |||||
Saudi SFDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Saudi SFDA approvals found for this drug. | |||||
Malaysia NPRA Drug Approvals
Approved Product | Company | Registration Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Malaysia NPRA approvals found for this drug. | |||||
UK EMC Drug Information
Medicine Name | MA Holder | MA Number | Pharmaceutical Form | Active Ingredient | Authorization Date |
|---|---|---|---|---|---|
| No UK EMC drug information found for this drug. | |||||
Help Us Improve
Your feedback helps us provide better drug information and insights.