Tìm theo
Etoricoxib
Các tên gọi khác (6 ) :
  • 5-chloro-2-(6-Methylpyridin-3-yl)-3-(4-(methylsulfonyl)phenyl)pyridine
  • 5-Chloro-3-(4-methanesulfonyl-phenyl)-6'-methyl-[2,3']bipyridinyl
  • 5-chloro-6'-Methyl-3-(P-(methylsulfonyl)phenyl)-2,3'-bipyridine
  • ETORICOXIB
  • Etoricoxibum
  • L791456
Thuốc Gốc
Small Molecule
CAS: 202409-33-4
ATC: M01AH05
CTHH: C18H15ClN2O2S
PTK: 358.842
Etoricoxib is a new COX-2 selective inhibitor. Current therapeutic indications are: treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, chronic low back pain, acute pain and gout. Like any other COX-2 selective inhibitor, Etoricoxib selectively inhibits isoform 2 of cyclo-oxigenase enzyme (COX-2). This reduces the generation of prostaglandins (PGs) from arachidonic acid.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C18H15ClN2O2S
Phân tử khối
358.842
Monoisotopic mass
358.054276131
InChI
InChI=1S/C18H15ClN2O2S/c1-12-3-4-14(10-20-12)18-17(9-15(19)11-21-18)13-5-7-16(8-6-13)24(2,22)23/h3-11H,1-2H3
InChI Key
InChIKey=MNJVRJDLRVPLFE-UHFFFAOYSA-N
IUPAC Name
5-chloro-3-(4-methanesulfonylphenyl)-2-(6-methylpyridin-3-yl)pyridine
Traditional IUPAC Name
etoricoxib
SMILES
CC1=NC=C(C=C1)C1=C(C=C(Cl)C=N1)C1=CC=C(C=C1)S(C)(=O)=O
Độ hòa tan
3.28e-03 g/l
logP
2.79
logS
-5
pKa (strongest acidic)
19.69
pKa (Strongest Basic)
4.96
PSA
59.92 Å2
Refractivity
95.04 m3·mol-1
Polarizability
36.42 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
4
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Etoricoxib is a COX-2 selective inhibitor (approximately 106 times more selective for COX-2 inhibition over COX-1). Currently it is approved in more than 60 countries worldwide but not in the US, where the Food and Drug Administration (FDA) require additional safety and efficacy data for etoricoxib before it will issue approval.
Cơ Chế Tác Dụng : Etoricoxib is a new COX-2 selective inhibitor. Current therapeutic indications are: treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, chronic low back pain, acute pain and gout. Like any other COX-2 selective inhibitor, Etoricoxib selectively inhibits isoform 2 of cyclo-oxigenase enzyme (COX-2). This reduces the generation of prostaglandins (PGs) from arachidonic acid. Like any other COX-2 selective inhibitor Etoricoxib selectively inhibits isoform 2 of cyclo-oxigenase enzyme (COX-2). This reduces prostaglandins (PGs) generation from arachidonic acid.
Dược Động Học :
▧ Absorption :
Bioavailability is 100% following oral administration.
▧ Protein binding :
92%
▧ Metabolism :
Hepatic, primarily via CYP3A4.
▧ Half Life :
22 hours
Độc Tính : This reduced activity is the cause of reduced gastrointestinal toxicity, as demonstrated in several large clinical trials performed with different COXIB (see below links on NEJM and The Lancet). Some clinical trials and meta-analysis showed that treatment with COXIB lead to increased incidence of cardiovascular adverse events compared to placebo
Chỉ Định : For the treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, chronic low back pain, acute pain and gout.
Tương Tác Thuốc :
  • Acenocoumarol Etoricoxib may increase the anticoagulant effect of acenocoumarol.
  • Anisindione Etoricoxib may increase the anticoagulant effect of anisindione.
  • Dicoumarol Etoricoxib may increase the anticoagulant effect of dicumarol.
  • Ethinyl Estradiol Etoricoxib may increase the levels of ethinyl estradiol.
  • Lithium Etoricoxib increases serum levels of lithium
  • Rifampicin Rifampin reduces levels and efficacy of etoricoxib
  • Warfarin Etoricoxib may increase the anticoagulant effect of warfarin.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Algix
  • Công ty :
    Sản phẩm biệt dược : Arcoxia
  • Sản phẩm biệt dược : Coxyveen
  • Công ty :
    Sản phẩm biệt dược : Etorix
  • Công ty :
    Sản phẩm biệt dược : Nucoxia
  • Công ty :
    Sản phẩm biệt dược : Tauxib
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01628
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=123619
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504505
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C11718
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D03710
ChemSpider
http://www.chemspider.com/Chemical-Structure.110209.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50072064
PharmGKB
http://www.pharmgkb.org/drug/PA164776853
Wikipedia
http://en.wikipedia.org/wiki/Etoricoxib
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