Effects of monomethyl fumarate: A Synthesis of Findings from 23 Studies

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Original Abstract of the Article

Major Research Findings

Monomethyl fumarate (MMF) is an active metabolite of dimethyl fumarate (DMF) and is approved for the treatment of multiple sclerosis (MS). 6 , 5 , 20 , 15 , 22 , 12 , 19 , 18 , 16 , 14 , 23 , 7 , 3 , 13 , 9 . Research suggests that MMF acts on GPR109A receptors on immune cells, thus suppressing inflammatory responses and exhibiting immunomodulatory effects. 6 . MMF has been shown to suppress transplant rejection by converting dendritic cells into tolerogenic dendritic cells. 5 . MMF is reported to induce changes in the peripheral neutrophil compartment of psoriasis patients, which is linked to skin improvement. 20 . DMF can cause skin sensitization, which makes topical application difficult. However, a new DMF derivative, isosorbide DMF (IDMF), has been shown to be effective for psoriasis without causing sensitization. 15 . MMF has been reported to improve murine macrophage activation syndrome (MAS) in both heme oxygenase 1 (HO-1)-dependent and HO-1-independent manners. 22 . DMF has been shown to exert neuroprotective effects against depression-like behaviors through modulation of astrocytes and microglia in mice. 10 . Sodium butyrate (NaB) and MMF have been shown to exert neuroprotective effects in PD mice by modulating GPR109A and restoring intestinal barrier function. 1 . CBD combined with angiotensin receptor blockers (ARBs) effectively inhibits glial nitric oxide release, suggesting a promising strategy for neuroinflammation treatment. 2 . Itaconate and fumarate derivatives have been shown to inhibit the priming and activation of the canonical NLRP3 inflammasome in macrophages. 14 . DMF has been shown to inhibit the growth of MCPyV-negative Merkel cell carcinoma cell lines. 9 .

Benefits and Risks

Benefits Summary

Monomethyl fumarate (MMF) is approved for the treatment of multiple sclerosis (MS) and shows promise for psoriasis and other inflammatory diseases. 6 , 5 , 20 , 15 , 22 , 12 , 19 , 18 , 16 , 14 , 23 , 7 , 3 , 13 , 9 . MMF acts on GPR109A receptors on immune cells to suppress inflammatory responses and exhibit immunomodulatory effects. 6 . It can also convert dendritic cells into tolerogenic dendritic cells to suppress transplant rejection. 5 . DMF can cause skin sensitization, making topical application difficult. However, a new DMF derivative, isosorbide DMF (IDMF), has been shown to be effective for psoriasis without causing sensitization. 15 . Furthermore, MMF has been reported to improve murine macrophage activation syndrome (MAS) in both heme oxygenase 1 (HO-1)-dependent and HO-1-independent manners. 22 . DMF has been shown to exert neuroprotective effects against depression-like behaviors through modulation of astrocytes and microglia in mice. 10 . Sodium butyrate (NaB) and MMF have been shown to exert neuroprotective effects in PD mice by modulating GPR109A and restoring intestinal barrier function. 1 . CBD combined with angiotensin receptor blockers (ARBs) effectively inhibits glial nitric oxide release, suggesting a promising strategy for neuroinflammation treatment. 2 . Itaconate and fumarate derivatives have been shown to inhibit the priming and activation of the canonical NLRP3 inflammasome in macrophages. 14 . DMF has been shown to inhibit the growth of MCPyV-negative Merkel cell carcinoma cell lines. 9 .

Risks Summary

DMF has been reported to cause lymphopenia. 23 . DMF can cause gastrointestinal side effects, but DRF has been reported to have fewer side effects compared to DMF. 3 .

Research Comparison

Research Similarities

Multiple studies have shown that MMF acts on GPR109A receptors on immune cells, thus suppressing inflammatory responses and exhibiting immunomodulatory effects. 6 . MMF has been shown to suppress transplant rejection by converting dendritic cells into tolerogenic dendritic cells. 5 . These studies suggest that MMF could be effective in treating various inflammatory diseases.

Research Differences

There are differences in the mechanism of action and effectiveness of MMF across studies. For instance, DMF can cause skin sensitization, which makes topical application difficult. However, a new DMF derivative, isosorbide DMF (IDMF), has been shown to be effective for psoriasis without causing sensitization. 15 . Also, MMF has been reported to improve murine macrophage activation syndrome (MAS) in both heme oxygenase 1 (HO-1)-dependent and HO-1-independent manners. 22 . Furthermore, DMF has been shown to exert neuroprotective effects against depression-like behaviors through modulation of astrocytes and microglia in mice. 10 . These studies suggest the broad therapeutic potential of MMF, but further research is needed.

Consistency and Contradictions of Results

Multiple research findings have suggested that MMF is a promising therapeutic agent for various inflammatory diseases. 6 , 5 , 20 , 15 , 22 , 12 , 19 , 18 , 16 , 14 , 23 , 7 , 3 , 13 , 9 . However, there are differences in the mechanism of action and effectiveness of MMF, which highlights the need for further research.

Considerations for Real-World Applications

MMF shows promise as a medication for inflammatory diseases such as multiple sclerosis and psoriasis. 6 , 5 , 20 , 15 . However, MMF can cause lymphopenia and may have gastrointestinal side effects. 23 , 3 . Therefore, it is critical to follow a doctor's instructions when using MMF.

Limitations of Current Research

Research on MMF is still in its early stages and further research is needed. 6 , 5 , 20 , 15 , 22 , 12 , 19 , 18 , 16 , 14 , 23 , 7 , 3 , 13 , 9 . Further research is needed on the long-term effects and side effects of MMF, as well as its effectiveness in various inflammatory diseases.

Future Directions for Research

MMF shows promise as a therapeutic agent for various inflammatory diseases. 6 , 5 , 20 , 15 , 22 , 12 , 19 , 18 , 16 , 14 , 23 , 7 , 3 , 13 , 9 . However, there are differences in the mechanism of action and effectiveness of MMF, which highlights the need for further research. Future studies should investigate the long-term effects and side effects of MMF, as well as its effectiveness in various inflammatory diseases.

Conclusion

Monomethyl fumarate (MMF) is approved for the treatment of multiple sclerosis (MS) and shows promise for psoriasis and other inflammatory diseases. 6 , 5 , 20 , 15 , 22 , 12 , 19 , 18 , 16 , 14 , 23 , 7 , 3 , 13 , 9 . MMF acts on GPR109A receptors on immune cells to suppress inflammatory responses and exhibit immunomodulatory effects. 6 . However, MMF can cause lymphopenia and may have gastrointestinal side effects. 23 , 3 . It is important to follow a doctor's instructions when using MMF.

Literature analysis of 23 papers
Positive Content
22
Neutral Content
1
Negative Content
0
Article Type
1
0
0
3
23
3.

Diroximel fumarate in patients with relapsing-remitting multiple sclerosis: Final safety and efficacy results from the phase 3 EVOLVE-MS-1 study.

Author: SingerBarry A, ArnoldDouglas L, DrulovicJelena, FreedmanMark S, GoldRalf, GudesblattMark, JasinskaElzbieta, LaGankeChristopher C, NaismithRobert T, NegroskiDonald, OhJiwon, Hernandez PerezMiguel Angel, SelmajKrzysztof, Then BerghFlorian, WundesAnnette, ZiemssenTjalf, Castro-BorreroWanda, ChenHailu, LevinSeth, ScaramozzaMatthew, ShankarSai L, WangTing, WraySibyl

Reduced GI side effects

Diroximel fumarate (DRF) is approved for the treatment of multiple sclerosis (MS) and has been shown to have fewer gastrointestinal (GI) side effects compared to dimethyl fumarate (DMF).

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

4.

Biased allosteric activation of ketone body receptor HCAR2 suppresses inflammation.

Author: ZhaoChang, WangHeli, LiuYing, ChengLin, WangBo, TianXiaowen, FuHong, WuChao, LiZiyan, ShenChenglong, YuJingjing, YangShengyong, HuHongbo, FuPing, MaLiang, WangChuanxin, YanWei, ShaoZhenhua

Anti-inflammatory efficacy
HCAR2 modulation

Compound 9n is a G<sub>i</sub>-biased allosteric modulator (BAM) of HCAR2. This study characterized compound 9n as a BAM of HCAR2 and demonstrated its anti-inflammatory efficacy in macrophages. The study also revealed the structural basis of compound 9n's action.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

6.

Immune cell targeted fumaric esters support a role of GPR109A as a primary target of monomethyl fumarate in vivo.

Author: StraßSimon, GeigerJohanna, CloosNatascha, SpäthNadja, GeigerSophia, SchwambornAnna, De Oliveira da CunhaLuciano, MartorelliMariella, GuseJan-Hinrich, SandriThaisa Lucas, BurnetMichael, LauferStefan

Immunomodulatory
Reduce cytokine levels

Dimethyl fumarate (DMF) is used to treat multiple sclerosis (MS), but its mode of action is unclear. This study suggests that monomethyl fumarate (MMF), a hydrolysis product of DMF, may be a more effective ligand to GPR109A, a receptor involved in immune cell function, than DMF itself.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

8.

Experimental Investigations of Monomethyl and Dimethyl Fumarate in an Astrocyte-Microglia Co-Culture Model of Inflammation.

Author: CorvaceFranco, FaustmannTimo Jendrik, HeckersSandra, FaustmannPedro M, IsmailFatme Seval

MS treatment

This study investigates the effects of dimethyl fumarate (DMF) and monomethyl fumarate (MMF) on microglial activation, morphology, glial viability, Cx43, and AQP4 expressions in an in vitro astrocyte-microglia co-culture model of inflammation.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

10.

Neuroprotective effects of dimethyl fumarate against depression-like behaviors via astrocytes and microglia modulation in mice: possible involvement of the HCAR2/Nrf2 signaling pathway.

Author: de SouzaAlana Gomes, LopesIardja Stéfane, FilhoAdriano José Maia Chaves, CavalcanteTalita Matias Barbosa, OliveiraJoão Victor Souza, de CarvalhoMichele Albuquerque Jales, de LimaKlistenes Alves, JucáPaloma Marinho, MendonçaSabrina Silva, MottinMelina, AndradeCarolina Horta, de SousaFrancisca Cléa Florenço, MacedoDanielle S, de França FontelesMarta Maria

Neuroprotective effects

This study found that dimethyl fumarate (DMF) can exert neuroprotective effects against depression-like behaviors by modulating astrocytes and microglia. DMF reversed CUMS-induced anxiety- and depressive-like behaviors and cognitive deficits, suggesting that its antidepressant effect may be mediated through neuroinflammatory suppression.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

12.

Dimethyl fumarate: A review of preclinical efficacy in models of neurodegenerative diseases.

Author: MajkutewiczIrena

Anti-inflammatory
Antioxidant
Neuroprotective

This review analyzes the neuroprotective, antioxidative, and anti-inflammatory effects of dimethyl fumarate (DMF) and its metabolite monomethyl fumarate (MMF) in various neurodegenerative diseases.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

16.

Dexamethasone and Fumaric Acid Ester Conjugate Synergistically Inhibits Inflammation and NF-κB in Macrophages.

Author: GenitoChristopher J, Eckshtain-LeviMeital, Piedra-QuinteroZayda L, KroviSai Archana, KrobothAbriana, StiepelRebeca T, Guerau-de-ArellanoMireia, BachelderEric M, AinslieKristy M

Autoimmune and chronic inflammatory disease treatment
Immune-dampening side effects

This study investigates the synergistic anti-inflammatory activity of a conjugate of dexamethasone and monomethyl fumarate in both murine and human macrophages. The conjugate shows promise for treating autoimmune and inflammatory diseases.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, N.I.H., ExtramuralResearch funding provided by the NIH to external research institutions and researchers.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

17.

Hydroxycarboxylic Acid Receptor 2, a Pleiotropically Linked Receptor for the Multiple Sclerosis Drug, Monomethyl Fumarate. Possible Implications for the Inflammatory Response.

Author: ParodiBenedetta, SannaAlessia, CedolaAlessia, UccelliAntonio, Kerlero de RosboNicole

Multiple sclerosis treatment
Gastrointestinal inflammation
Skin flushing

Monomethyl fumarate (MMF), a drug used for multiple sclerosis, activates different signaling pathways in different cell types through the HCAR2 receptor, potentially leading to both beneficial and inflammatory effects.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

19.

Pharmacokinetics and Bioavailability of Monomethyl Fumarate Following a Single Oral Dose of Bafiertam&#8482; (Monomethyl Fumarate) or Tecfidera<sup>&#174;</sup> (Dimethyl Fumarate).

Author: LateganThomas W, WangLaurene, SpragueTiffany N, RousseauFranck S

Bioequivalent
Effective treatment

Two Bafiertam™ capsules each containing 95 mg of MMF are bioequivalent to one Tecfidera™ 240 mg capsule in terms of pharmacokinetic parameters of MMF, including AUC, Cmax, and Tmax.

Comparative StudyResearch that compares multiple groups/interventions to determine differences/similarities in outcomes/characteristics.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

20.

Oral dimethyl fumarate induces changes within the peripheral neutrophil compartment of patients with psoriasis that are linked with skin improvement.

Author: MorrisonP J, SuhrkampI, GerdesS, MrowietzU

Improve skin inflammation

Dimethyl fumarate (DMF) is a drug that is used to treat psoriasis and multiple sclerosis. This review discusses the mechanism of action of DMF and its effects on the immune system.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

21.

Different Fumaric Acid Esters Elicit Distinct Pharmacologic Responses.

Author: WipkeBrian T, HoepnerRobert, Strassburger-KrogiasKatrin, ThomasAnkur M, GianniDavide, SzakSuzanne, BrennanMelanie S, PistorMaximilian, GoldRalf, ChanAndrew, ScannevinRobert H

This study investigates the biological effects of dimethyl fumarate (DMF) alone and in combination with monoethyl fumarate (MEF) in rodents and cynomolgus monkeys. The study aims to understand the distinct mechanisms of action of these two therapies and their potential implications for multiple sclerosis (MS) treatment.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Observational StudyResearch that observes and collects data on participants' behavior and outcomes in their natural state, without intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

22.

Amelioration of Murine Macrophage Activation Syndrome by Monomethyl Fumarate in Both a Heme Oxygenase 1-Dependent and Heme Oxygenase 1-Independent Manner.

Author: BiswasChhanda, ChuNiansheng, BurnThomas N, KreigerPortia A, BehrensEdward M

Amelioration of MAS disease activity

Monomethyl fumarate (MMF), the active metabolite of dimethyl fumarate, shows promise in treating macrophage activation syndrome (MAS), a life-threatening complication of autoimmune disorders. MMF activates heme oxygenase 1 (HO-1), which has anti-inflammatory properties. Further research is needed to evaluate the efficacy of MMF in treating MAS.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, N.I.H., ExtramuralResearch funding provided by the NIH to external research institutions and researchers.

Language : English

23.

Dimethyl fumarate induced lymphopenia in multiple sclerosis: A review of the literature.

Author: Dello RussoCinzia, ScottKathryn Anne, PirmohamedMunir

MS treatment
Lymphopenia
Progressive multifocal leukoencephalopathy

This review discussed the molecular mechanisms underlying dimethyl fumarate (DMF)-induced lymphopenia, a potential side effect of DMF treatment for multiple sclerosis.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

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