Tìm theo
MACITENTAN
Các tên gọi khác (5 ) :
  • ACT 064992
  • ACT-064992
  • ACT064992
  • Macitentanum
  • OPSUMIT
Thuốc tim mạch
Thuốc Gốc
Small Molecule
CAS: 441798-33-0
CTHH: C19H20Br2N6O4S
PTK: 588.273
Macitentan was approved in October 2013. It is indicated for patients with pulmonary arterial hypertension, and is marketed under the brand name Opsumit. Macitentan is an antagonist/blocker of endothelin receptors on blood vessels and smooth muscle, and, thus, blocks the stimulation of vasculature hypertrophy, inflammation, fibrosis, proliferation, and vasoconstriction. Similar to all drugs acting on the renin-angiotensin system, macitentan is associated with embryo and fetal toxicity, so it should not be used in pregnancy and has special precautions that must be followed for all females of child-bearing age.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H20Br2N6O4S
Phân tử khối
588.273
Monoisotopic mass
585.963349142
InChI
InChI=1S/C19H20Br2N6O4S/c1-2-7-26-32(28,29)27-17-16(13-3-5-14(20)6-4-13)18(25-12-24-17)30-8-9-31-19-22-10-15(21)11-23-19/h3-6,10-12,26H,2,7-9H2,1H3,(H,24,25,27)
InChI Key
InChIKey=JGCMEBMXRHSZKX-UHFFFAOYSA-N
IUPAC Name
{[5-(4-bromophenyl)-6-{2-[(5-bromopyrimidin-2-yl)oxy]ethoxy}pyrimidin-4-yl]sulfamoyl}(propyl)amine
Traditional IUPAC Name
{[5-(4-bromophenyl)-6-{2-[(5-bromopyrimidin-2-yl)oxy]ethoxy}pyrimidin-4-yl]sulfamoyl}(propyl)amine
SMILES
CCCNS(=O)(=O)NC1=C(C(OCCOC2=NC=C(Br)C=N2)=NC=N1)C1=CC=C(Br)C=C1
Độ hòa tan
Not water soluble
logP
3.69
logS
-4.9
pKa (strongest acidic)
7.76
pKa (Strongest Basic)
2.26
PSA
128.22 Å2
Refractivity
126.98 m3·mol-1
Polarizability
50.55 Å3
Rotatable Bond Count
9
H Bond Acceptor Count
9
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
3
Bioavailability
1
MDDR-Like Rule
true
Dược Lực Học : Macitentan blocks simulators of hypertrophy, inflammation, fibrosis, proliferation, and vasoconstriction.
Cơ Chế Tác Dụng : Macitentan was approved in October 2013. It is indicated for patients with pulmonary arterial hypertension, and is marketed under the brand name Opsumit. Macitentan is an antagonist/blocker of endothelin receptors on blood vessels and smooth muscle, and, thus, blocks the stimulation of vasculature hypertrophy, inflammation, fibrosis, proliferation, and vasoconstriction. Similar to all drugs acting on the renin-angiotensin system, macitentan is associated with embryo and fetal toxicity, so it should not be used in pregnancy and has special precautions that must be followed for all females of child-bearing age. Macitentan is an antagonist/blocker of endothelin receptors. Endothelin receptors are found in the endothelial cells of blood vessels and smooth muscle. Macitentan binds to the receptors, endothelin A and B (ETA and ETB), which prevents the agonist endothelin -1 (ET-1) from binding and stimulating the ETA and ETB receptors.
Dược Động Học :
▧ Absorption :
Macitentan is administered orally, and it take about 8 hours for maximum plasma concentrations to be reached.
▧ Volume of Distribution :
Macitentan has a volume of distribution of 50L.
▧ Protein binding :
Macitentan is >99% bound to plasma proteins, which are mainly albumin
▧ Metabolism :
Macitentan is metabolised to an active metabolite by CYP 3A4 (major) and CYP 2C19 (minor).
▧ Route of Elimination :
Eliminated 50% through urine and 24% through feces.
▧ Half Life :
The half life of macitentan is 16 hours, and the half life of it's active metabolite is 48 hours.
▧ Clearance :
Clearance data was not found.
Độc Tính : Macitentan has a black box warning of embryo-fetal toxicity. Special precautions must be taken for all females of child-bearing age, and women who are pregnant must not be given macitentan.
Chỉ Định : Macitentan is indicated for patients with pulmonary arterial hypertension.
Liều Lượng & Cách Dùng : Tablet - Oral - 10 MG
Dữ Kiện Thương Mại
Nhà Sản Xuất
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08932
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D10135
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/66215-501-30
Wikipedia
http://en.wikipedia.org/wiki/Macitentan
RxList
http://www.rxlist.com/opsumit-drug.htm
Drugs.com
http://www.drugs.com/cons/macitentan.html
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