Tìm theo
Icosapent ethyl
Các tên gọi khác (8 ) :
  • EPA ethyl ester
  • Epadel S
  • Ethyl Eicosapentaenoate
  • Ethyl icosapentate
  • Ethyl-Eicosapentaenoic Acid
  • Ethyl-EPA
  • Icosapent ethyl
  • Vascepa
hypolipidemic agents
Thuốc Gốc
Small Molecule
CAS: 86227-47-6
CTHH: C22H34O2
PTK: 330.5042
Icosapent ethyl or ethyl eicosapentaenoic acid is a synthetic derivative of the omega-3 fatty acid eicosapentaenoic acid (EPA). It is used as adjunct therapy for severe hypertriglyceridemia (TG levels > 500 mg/dL). FDA approved on July 26, 2012.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C22H34O2
Phân tử khối
330.5042
Monoisotopic mass
330.255880332
InChI
InChI=1S/C22H34O2/c1-3-5-6-7-8-9-10-11-12-13-14-15-16-17-18-19-20-21-22(23)24-4-2/h5-6,8-9,11-12,14-15,17-18H,3-4,7,10,13,16,19-21H2,1-2H3/b6-5-,9-8-,12-11-,15-14-,18-17-
InChI Key
InChIKey=SSQPWTVBQMWLSZ-AAQCHOMXSA-N
IUPAC Name
ethyl (5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenoate
Traditional IUPAC Name
ethyl eicosapentaenoate
SMILES
CCOC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/C\C=C/CC
Độ hòa tan
9.83e-05 g/l
logP
6.73
logS
-6.5
pKa (Strongest Basic)
-7
PSA
26.3 Å2
Refractivity
110.59 m3·mol-1
Polarizability
40.4 Å3
Rotatable Bond Count
15
H Bond Acceptor Count
1
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
0
Bioavailability
0
Cơ Chế Tác Dụng : Icosapent ethyl or ethyl eicosapentaenoic acid is a synthetic derivative of the omega-3 fatty acid eicosapentaenoic acid (EPA). It is used as adjunct therapy for severe hypertriglyceridemia (TG levels > 500 mg/dL). FDA approved on July 26, 2012. Studies suggest that EPA reduces hepatic very low-density lipoprotein triglycerides (VLDL-TG) synthesis and/or secretion and enhances TG clearance from circulating VLDL particles. Potential mechanisms of action include increased β-oxidation; inhibition of acyl-CoA:1,2-diacylglycerol acyltransferase (DGAT); decreased lipogenesis in the liver; and increased plasma lipoprotein lipase activity.
Dược Động Học :
▧ Absorption :
Icosapent ethyl is de-esterfied, converted into active EPA, and then absorbed in the small intestine. It reaches peak plasma concentration in 5 hours post-oral administration. Very little (<1%) is left circulating in the plasma as EPA incorporates into phospholipids, TG's, and cholesteryl esters.
▧ Volume of Distribution :
Steady state volume of distribution of active EPA is 88 L
▧ Metabolism :
Once converted into active EPA, it is hepatically metabolized into acetyl Coenzyme A via beta-oxidation.
▧ Route of Elimination :
Icosapent ethyl is not renally excreted
▧ Half Life :
The half life of EPA is 89 hours.
▧ Clearance :
Total plasma clearance, EPA = 684 mL/hr
Độc Tính : Icosapent ethyl is generally well tolerated and adverse effects are unrelated to treatment.
Chỉ Định : Icosapent ethyl is used as adjunct therapy to reduce triglyceride (TG) levels in adults with severe (>500 mg/dL) hypertriglyceridemia.
Liều Lượng & Cách Dùng : Capsule - Oral - 1 g
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Epadel
  • Sản phẩm biệt dược : Vascepa
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08887
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C16184
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01892
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/52937-001-04
Wikipedia
http://en.wikipedia.org/wiki/Ethyl_eicosapentaenoic_acid
RxList
http://www.rxlist.com/vascepa-drug.htm
Drugs.com
http://www.drugs.com/cdi/icosapent-ethyl.html
... loading
... loading