Peringatan Keamanan

Cases of overdose with dimethyl fumarate have been reported, and symptoms were consistent with its adverse event profile. There are no known therapeutic interventions to enhance dimethyl fumarate elimination nor an antidote. The product label of dimethyl fumarate recommends initiating symptomatic supportive treatment as clinically indicated in case of overdose.L43752 In vivo carcinogenicity studies found that at doses ranging between 200 and 400 mg/kg/day, mice had a higher incidence of non-glandular stomach and kidney tumors. The highest dose not associated with tumors in mice (75 mg/kg/day) is equivalent to the recommended human dose (RHD) of 480 mg/day.L43752 Dimethyl fumarate did not show evidence of mutagenicity in the in vitro bacterial reverse mutation (Ames) assay. Dimethyl fumarate was clastogenic in the in vitro chromosomal aberration assay in human peripheral blood lymphocytes in the absence of metabolic activation, but not clastogenic in the in vivo micronucleus assay in the rat.L43752

Dimethyl fumarate

DB08908

small molecule approved investigational

Deskripsi

Dimethyl fumarate is an agent indicated for the treatment of relapsing forms of multiple sclerosis.A253942,L43752 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.L43752 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.A253917 Prior to its FDA approval, dimethyl fumarate had been used in Germany for treatment of psoriasis.A253917

Struktur Molekul 2D

Berat 144.1253
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The dimethyl fumarate metabolite monomethyl fumarate (MMF) has a short half-life of about 1 hour. MMF does not accumulate after repeated doses of dimethyl fumarate.[L43752]
Volume Distribusi In healthy people, monomethyl fumarate (MMF) has a variable volume of distribution of 53 to 73 litres.[L43757]
Klirens (Clearance) Monomethyl fumarate (MMF), the active metabolite of dimethyl fumarate, has a rapid clearance. Its apparent clearance (Cl/F) appears to be dose-independent.[L43757]

Absorpsi

Once ingested, dimethyl fumarate is rapidly hydrolyzed by esterases to form monomethyl fumarate (MMF). Therefore, there is a negligible amount of dimethyl fumarate in the body, and all pharmacokinetic information is quantified with MMF.L43752 The time to maximum concentration (tmax) of MMF ranges between 2 and 2.5 hours. In patients with multiple sclerosis given 240 mg of dimethyl fumarate two times a day with food, the Cmax and AUC were 1.87 mg/L and 8.21 mg?hr/L, respectively. High-fat, high-calorie meals decrease the Cmax of MMF by 40% and cause a tmax delay from 2 hours to 5.5 hours; however, these changes are not considered clinically significant.L43752

Metabolisme

Dimethyl fumarate is quickly hydrolyzed by esterases in the gastrointestinal tract, tissues, and blood to form monomethyl fumarate (MMF), its active metabolite. MMF then undergoes subsequent metabolism through the tricarboxylic acid (TCA) cycle. The main metabolites of dimethyl fumarate are MMF, glucose, citric, and fumaric acid. Cytochrome P450 (CYP) enzymes do not participate in the metabolism of dimethyl fumarate.L43757

Rute Eliminasi

The main route of elimination of dimethyl fumarate is by CO2 exhalation, which accounts for 60% of the dose. The other minor routes of elimination are through the kidney (16% of the dose) and feces (1% of the dose). Trace amounts of unchanged monomethyl fumarate (the active metabolite of dimethyl fumarate) are present in urine.L43757

Interaksi Makanan

1 Data
  • 1. Take with or without food. The incidence of flushing may be reduced by the administration of dimethyl fumarate with food; however, the product label states that it may be taken with or without food.

Interaksi Obat

353 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Dimethyl fumarate.
Etanercept The risk or severity of adverse effects can be increased when Etanercept is combined with Dimethyl fumarate.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Dimethyl fumarate.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Dimethyl fumarate.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Dimethyl fumarate.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Dimethyl fumarate.
Anakinra The risk or severity of adverse effects can be increased when Anakinra is combined with Dimethyl fumarate.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Dimethyl fumarate.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Dimethyl fumarate.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Dimethyl fumarate.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Dimethyl fumarate.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Dimethyl fumarate.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Dimethyl fumarate.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Dimethyl fumarate.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Dimethyl fumarate.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Dimethyl fumarate.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Dimethyl fumarate.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Dimethyl fumarate.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Dimethyl fumarate.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Dimethyl fumarate.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Dimethyl fumarate.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Dimethyl fumarate.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Dimethyl fumarate.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Dimethyl fumarate.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Dimethyl fumarate.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Dimethyl fumarate.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Dimethyl fumarate.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Dimethyl fumarate.
Flunisolide The risk or severity of adverse effects can be increased when Flunisolide is combined with Dimethyl fumarate.
Bortezomib The risk or severity of adverse effects can be increased when Bortezomib is combined with Dimethyl fumarate.
Cladribine Dimethyl fumarate may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Dimethyl fumarate.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Dimethyl fumarate.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Dimethyl fumarate.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Dimethyl fumarate.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Dimethyl fumarate.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Dimethyl fumarate.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Dimethyl fumarate.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Dimethyl fumarate.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Dimethyl fumarate.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Dimethyl fumarate.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Dimethyl fumarate.
Vinorelbine The risk or severity of adverse effects can be increased when Vinorelbine is combined with Dimethyl fumarate.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Dimethyl fumarate.
Beclomethasone dipropionate The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Dimethyl fumarate.
Sorafenib The risk or severity of adverse effects can be increased when Sorafenib is combined with Dimethyl fumarate.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Dimethyl fumarate.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Dimethyl fumarate.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Dimethyl fumarate.
Betamethasone The risk or severity of adverse effects can be increased when Betamethasone is combined with Dimethyl fumarate.
Teniposide The risk or severity of adverse effects can be increased when Teniposide is combined with Dimethyl fumarate.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Dimethyl fumarate.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Dimethyl fumarate.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Dimethyl fumarate.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Dimethyl fumarate.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Dimethyl fumarate.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Dimethyl fumarate.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Dimethyl fumarate.
Cyclophosphamide The risk or severity of adverse effects can be increased when Cyclophosphamide is combined with Dimethyl fumarate.
Vincristine The risk or severity of adverse effects can be increased when Vincristine is combined with Dimethyl fumarate.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Dimethyl fumarate.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Dimethyl fumarate.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Dimethyl fumarate.
Methotrexate The risk or severity of adverse effects can be increased when Methotrexate is combined with Dimethyl fumarate.
Carbamazepine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Dimethyl fumarate.
Vinblastine The risk or severity of adverse effects can be increased when Vinblastine is combined with Dimethyl fumarate.
Fluticasone propionate The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Dimethyl fumarate.
Fluocinolone acetonide The risk or severity of adverse effects can be increased when Fluocinolone acetonide is combined with Dimethyl fumarate.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Dimethyl fumarate.
Imatinib The risk or severity of adverse effects can be increased when Imatinib is combined with Dimethyl fumarate.
Triamcinolone The risk or severity of adverse effects can be increased when Triamcinolone is combined with Dimethyl fumarate.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Dimethyl fumarate.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Dimethyl fumarate.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Dimethyl fumarate.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Dimethyl fumarate.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Dimethyl fumarate.
Daunorubicin The risk or severity of adverse effects can be increased when Daunorubicin is combined with Dimethyl fumarate.
Irinotecan The risk or severity of adverse effects can be increased when Irinotecan is combined with Dimethyl fumarate.
Methimazole The risk or severity of adverse effects can be increased when Methimazole is combined with Dimethyl fumarate.
Etoposide The risk or severity of adverse effects can be increased when Etoposide is combined with Dimethyl fumarate.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Dimethyl fumarate.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Dimethyl fumarate.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Dimethyl fumarate.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Dimethyl fumarate.
Prednisolone The risk or severity of adverse effects can be increased when Prednisolone is combined with Dimethyl fumarate.
Sirolimus The risk or severity of adverse effects can be increased when Sirolimus is combined with Dimethyl fumarate.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Dimethyl fumarate.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Dimethyl fumarate.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Dimethyl fumarate.
Methylprednisolone The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Dimethyl fumarate.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Dimethyl fumarate.
Cytarabine The risk or severity of adverse effects can be increased when Cytarabine is combined with Dimethyl fumarate.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Dimethyl fumarate.
Doxorubicin The risk or severity of adverse effects can be increased when Doxorubicin is combined with Dimethyl fumarate.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Dimethyl fumarate.
Busulfan The risk or severity of adverse effects can be increased when Busulfan is combined with Dimethyl fumarate.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Dimethyl fumarate.
Topotecan The risk or severity of adverse effects can be increased when Topotecan is combined with Dimethyl fumarate.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Dimethyl fumarate.
Thalidomide The risk or severity of adverse effects can be increased when Thalidomide is combined with Dimethyl fumarate.

Target Protein

Kelch-like ECH-associated protein 1 KEAP1
Transcription factor p65 RELA

Referensi & Sumber

Synthesis reference: Pullagurla, MR., et al. (2020). Process for the synthesis of dimethyl fumarate (U.S. Patent No. US 10,626,076 B2). U.S. Patent and Trademark Office. https://patentimages.storage.googleapis.com/37/67/f2/c406d1a9840dac/US10626076.pdf
Artikel (PubMed)
  • PMID: 21067468
    Papadopoulou A, D'Souza M, Kappos L, Yaldizli O: Dimethyl fumarate for multiple sclerosis. Expert Opin Investig Drugs. 2010 Dec;19(12):1603-12. doi: 10.1517/13543784.2010.534778. Epub 2010 Nov 11.
  • PMID: 24259625
    Venci JV, Gandhi MA: Dimethyl fumarate (Tecfidera): a new oral agent for multiple sclerosis. Ann Pharmacother. 2013 Dec;47(12):1697-702. doi: 10.1177/1060028013509232. Epub 2013 Oct 23.
  • PMID: 31784875
    Blair HA: Dimethyl Fumarate: A Review in Relapsing-Remitting MS. Drugs. 2019 Dec;79(18):1965-1976. doi: 10.1007/s40265-019-01229-3.

Contoh Produk & Brand

Produk: 161 • International brands: 0
Produk
  • Ach-dimethyl Fumarate
    Capsule, delayed release • 120 mg • Oral • Canada • Generic • Approved
  • Ach-dimethyl Fumarate
    Capsule, delayed release • 240 mg • Oral • Canada • Generic • Approved
  • Apo-dimethyl Fumarate
    Capsule, delayed release • 120 mg • Oral • Canada • Generic • Approved
  • Apo-dimethyl Fumarate
    Capsule, delayed release • 240 mg • Oral • Canada • Generic • Approved
  • Auro-dimethyl Fumarate
    Capsule, delayed release • 120 mg • Oral • Canada • Generic • Approved
  • Auro-dimethyl Fumarate
    Capsule, delayed release • 240 mg • Oral • Canada • Generic • Approved
  • Dimethyl fumarate
    Capsule, delayed release • 120 mg/1 • Oral • US • Generic • Approved
  • Dimethyl fumarate
    Capsule, delayed release • 240 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 161 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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