Tìm theo
Mipomersen
Các tên gọi khác (4 ) :
  • ISIS-301012
  • Kynamro
  • Mipomersen
  • Mipomersen sodium
anticholesteremic agents, hypolipidemic agents, oligodeoxyribonucleotides antisense
Thuốc Gốc
Small Molecule
CAS: 629167-92-6
ATC: C10AX11
Mipomersen sodium, which was known as the investigational drug, isis-301012, is the salt form of a synthetic phosphorothioate oligonucleotide. Mipomersen sodium prevents the formation of apo B-100, resulting in a decrease in the levels of apolipoprotein B (apo B), low density lipoprotein (LDL), and total cholesterol. Mipomersen is indicated in patients with homozygous familial hypercholesterolemia as an adjunct to diet and other lipid-lowering medications. It is marketed under the brand name Kynamro in the United States, and the FDA label includes a black box warning of hepatoxicity. Specifically, elevations in the liver enzymes, i.e. transaminases, and in liver fat (hepatic steatosis) have been reported. Due to this serious risk of liver toxicity, mipomersen sodium is only available to patients under the restricted program called Kynamro™ Risk Evaluation and Mitigation Strategy program.
Dược Lực Học : Mipomersen sodium decreases the levels of apolipoprotein B (apo B), low density lipoprotein (LDL) non-high density lipoprotein-cholesterol, and total cholesterol.
Cơ Chế Tác Dụng : Mipomersen sodium, which was known as the investigational drug, isis-301012, is the salt form of a synthetic phosphorothioate oligonucleotide. Mipomersen sodium prevents the formation of apo B-100, resulting in a decrease in the levels of apolipoprotein B (apo B), low density lipoprotein (LDL), and total cholesterol. Mipomersen is indicated in patients with homozygous familial hypercholesterolemia as an adjunct to diet and other lipid-lowering medications. It is marketed under the brand name Kynamro in the United States, and the FDA label includes a black box warning of hepatoxicity. Specifically, elevations in the liver enzymes, i.e. transaminases, and in liver fat (hepatic steatosis) have been reported. Due to this serious risk of liver toxicity, mipomersen sodium is only available to patients under the restricted program called Kynamro™ Risk Evaluation and Mitigation Strategy program. Mipomersen binds to the mRNA that codes for apoB-100. This binding leads to double-stranded RNA, which is degraded by RNase H and prevents translation of the mRNA to form the apo B-100 protein.
Dược Động Học :
▧ Absorption :
The maximum mipomersen concentration is reached in about 3-4 hours after subcutaneous injection. Additionally the bioavailability of mipomersn is dose-dependant and ranges from 54%-78%.
▧ Volume of Distribution :
The volume of distribution for mipomersen was not quantified.
▧ Protein binding :
Plasma protein binding for mipomersen is greater than or equal to 90%.
▧ Metabolism :
Mipomersem is metabolized by endonucleases. Once degraded into shorter oligonucleotides, it is metabolized further by exonucleases.
▧ Route of Elimination :
24 hours after mipomersem administration, less than 4% of mipomersem and/or it's metabolites were excreted in the urine.
▧ Half Life :
Mipomersem has a very long half life of 1-2 months.
▧ Clearance :
Clearance of mipomersem was not quantified.
Độc Tính : The FDA label includes a black box warning of mipomersem induced hepatoxicity. Other less serious adverse effects include nausea, headache, fatigue, local injection site reactions, and flu-like symptoms.
Chỉ Định : Used in patients with homozygous familial hypercholesterolemia as an adjunct to diet and other lipid-lowering medications.
Tương Tác Thuốc :
  • Ethanol The combination of these drugs will likely enhance mipomersen related hepatotoxicity. Therefore patients using both these drugs, should limit their alcohol to a daily maximum of 1 drink (or equivalent).
Liều Lượng & Cách Dùng : Solution - Subcutaneous - 200MG/ML
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : GENZYME CORP
    Sản phẩm biệt dược : KYNAMRO
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB05528
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D08946
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/58468-0191-1
Wikipedia
http://en.wikipedia.org/wiki/Mipomersen
RxList
http://www.rxlist.com/kynamro-drug.htm
Drugs.com
http://www.drugs.com/mtm/mipomersen.html
... loading
... loading