Tìm theo
Dimethyl fumarate
Các tên gọi khác (9 ) :
  • (e)-But-2-enedioic acid dimethyl ester
  • 1,2-Bis(methoxycarbonyl)-trans-ethylene
  • BG-12
  • dimethyl (E) butenedioate
  • Dimethyl trans-ethylenedicarboxylate
  • Fumaric acid, dimethyl ester
  • Tecfidera
  • trans-1,2-Ethylenedicarboxylic acid dimethyl ester
  • trans-Butenedioic acid dimethyl ester
dermatologic agents, immunosuppressive agents, radiation sensitizing agents
Thuốc Gốc
Small Molecule
CAS: 624-49-7
Dimethyl fumarate is an anti-inflammatory. It is indicated for multiple sclerosis patients with relapsing forms and is also being investigated for the treatment of psoriasis. 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.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Độ tan chảy
103 to 104
Độ sôi
192 to 193
Độ hòa tan
Highly soluble in water.
Dược Lực Học : The physiological effects dimethyl fumarate has on the body is not well understood. It is known that dimethyl fumarate has anti-inflammatory and cytoprotective effects, which both are likely involved in its actions in multiple sclerosis patients.
Cơ Chế Tác Dụng : Dimethyl fumarate is an anti-inflammatory. It is indicated for multiple sclerosis patients with relapsing forms and is also being investigated for the treatment of psoriasis. 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. 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). MMF up-regulates the Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) pathway that is activated in response to oxidative stress. As well MMF is an agonist at the nicotinic acid receptor, but the relevance of this is not known.
Dược Động Học :
▧ Absorption :
Once ingested, dimethyl fumarate is rapidly hydroylyzed by esterases to MMF. Thus there is negligible amount of dimethyl fumarate in the body, and all pharmacokinetic information is quantified with MMF. In multiple sclerosis patients, the time to maximum concentration of MMF is 2 to 2.5 hours and the maximum concentration is 1.87 mg/L.
▧ Volume of Distribution :
In healthy people, MMF has a variable volume of distribution of 53 to 73 litres.
▧ Protein binding :
MMF has a plasma protein binding range of 27 to 45%, and the binding is concentration independent.
▧ Metabolism :
Dimethly fumarate is hydrozlied to its metabolite MMF in the GIT, tissues, and blood by esterases. MMF then undergoes subsequent metabolism in the tricarboxylic acid (TCA) cycle. Altogether the main metabolites formed are MMF, glucose, citric acid, and fumaric.
▧ Route of Elimination :
The main route of elimination is by CO2 exhalation that accounts for 60% of the dose. The other minor routes are through the kidney (16% metabolites and trace amounts of unchanged MMF) and the feces (1%).
▧ Half Life :
MMF has a short half life of about 1 hour, and MMF does not accumulate after repeated doses of dimethyl fumarate.
▧ Clearance :
MMF clearance was not quantified.
Độc Tính : The most common side effects observed were nausea, diarrhea, abdominal pain, and flushing.
Chỉ Định : Used in multiple sclerosis patients with relapsing forms.
Liều Lượng & Cách Dùng : Capsule, delayed release - Oral - 120MG
Capsule, delayed release - Oral - 240MG
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Biogen Idec
    Sản phẩm biệt dược : Tecfidera
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08908
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/64406-006-02
Wikipedia
http://en.wikipedia.org/wiki/Dimethyl_fumarate
RxList
http://www.rxlist.com/tecfidera-drug.htm
Drugs.com
http://www.drugs.com/cdi/dimethyl-fumarate.html
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