Tìm theo
Gadofosveset trisodium
Các tên gọi khác (4 ) :
  • Ablavar
  • Gadofosveset
  • MS-325
  • Vasovist
contrast media, diagnostic agents
Thuốc Gốc
Small Molecule
CAS: 193901-90-5
ATC: V08CA11
CTHH: C33H40GdN3Na3O15P
PTK: 975.87
Gadofosveset trisodium is an intravenous contrast agent used with magnetic resonance angiography(MRA), which is a non-invasive way of imaging blood vessels. The agent allows for the vascular system to be imaged more clearly by the MRA. In this way, gadofosveset trisodium is used to help diagnose certain disorders of the heart and blood vessels.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C33H40GdN3Na3O15P
Phân tử khối
975.87
Monoisotopic mass
976.113113695
InChI
InChI=1S/C33H44N3O14P.Gd.3Na.H2O/c37-28(38)18-34(15-16-35(19-29(39)40)20-30(41)42)17-26(36(21-31(43)44)22-32(45)46)23-49-51(47,48)50-27-11-13-33(14-12-27,24-7-3-1-4-8-24)25-9-5-2-6-10-25;;;;;/h1-10,26-27H,11-23H2,(H,37,38)(H,39,40)(H,41,42)(H,43,44)(H,45,46)(H,47,48);;;;;1H2/q;+3;3*+1;/p-6
InChI Key
InChIKey=PIZALBORPSCYJU-UHFFFAOYSA-H
IUPAC Name
gadolinium(3+) ion trisodium 2-{[1-({2-[bis(carboxylatomethyl)amino]ethyl}(carboxylatomethyl)amino)-3-[(4,4-diphenylcyclohexyl phosphonato)oxy]propan-2-yl](carboxylatomethyl)amino}acetate hydrate
Traditional IUPAC Name
gadolinium(3+) trisodium 2-{[1-({2-[bis(carboxylatomethyl)amino]ethyl}(carboxylatomethyl)amino)-3-[(4,4-diphenylcyclohexyl phosphonato)oxy]propan-2-yl](carboxylatomethyl)amino}acetate hydrate
SMILES
O.[Na+].[Na+].[Na+].[Gd+3].[O-]C(=O)CN(CCN(CC([O-])=O)CC([O-])=O)CC(COP([O-])(=O)OC1CCC(CC1)(C1=CC=CC=C1)C1=CC=CC=C1)N(CC([O-])=O)CC([O-])=O
logP
-1.2
pKa (strongest acidic)
0.78
pKa (Strongest Basic)
9.67
PSA
268.96 Å2
Refractivity
241.55 m3·mol-1
Polarizability
69.9 Å3
Rotatable Bond Count
23
H Bond Acceptor Count
15
H Bond Donor Count
0
Physiological Charge
-5
Number of Rings
3
Bioavailability
0
MDDR-Like Rule
true
Dược Lực Học : Gadofosveset causes signal enhancement by shortening the T1 of water molecules that interact with it. The contrast agent complex's rotation rate is the primary factor determining the magnitude of relaxation enhancement. This relaxation enhancement increase only occurs when bound to human serum albumin.
Cơ Chế Tác Dụng : Gadofosveset trisodium is an intravenous contrast agent used with magnetic resonance angiography(MRA), which is a non-invasive way of imaging blood vessels. The agent allows for the vascular system to be imaged more clearly by the MRA. In this way, gadofosveset trisodium is used to help diagnose certain disorders of the heart and blood vessels. Gadofosveset binds reversibly to endogenous serum albumin resulting in longer vascular residence time than non-protein binding contrast agents. The binding to serum albumin also increases the magnetic resonance relaxivity of gadofosveset and decreases the relaxation time (Tl) of water protons resulting in an increase in signal intensity (brightness) of blood.
Dược Động Học :

▧ Volume of Distribution :
48 ± 16 mL/kg
▧ Protein binding :
80-90%
▧ Metabolism :
Gadofosveset does not undergo measurable metabolism.
▧ Route of Elimination :
Gadofosveset is eliminated primarily in the urine with approximately 83.5% of an injected dose excreted in the urine over 14 days. Ninety-four percent (94%) of urinary excretion occurs in the first 72 hours. A small portion of gadofosveset dose is recovered in feces (approximately 4.7%).
▧ Half Life :
18.5 hours
▧ Clearance :
6.57 ± 0.97 mL/h/kg following the administration of 0.03 mmol/kg.
Độc Tính : Gadolinium-based contrast agents increase the risk for nephrogenic systemic fibrosis (NSF) in patients with acute or chronic severe renal insufficiency (glomerular filtration rate < 30 mL/min/1.73m²).
Chỉ Định : Gadofosveset trisodium is indicated for use as a contrast agent in magnetic resonance angiography (MRA) to evaluate aortoiliac occlusive disease (AIOD) in adults with known or suspected peripheral vascular disease.
Tương Tác Thuốc :
  • Artemether Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Lumefantrine Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Warfarin In a clinical trial of 10 patients receiving a stable dose of warfarin, a single dose of ABLAVAR (0.05 mmol/kg) did not alter the anticoagulant activity of warfarin as measured by the International Normalized Ratio (INR).
Liều Lượng & Cách Dùng : Solution - Intravenous - 0.03 mmol/kg
Dữ Kiện Thương Mại
Nhà Sản Xuất
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB06705
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D04286
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/11994-012-01
PharmGKB
http://www.pharmgkb.org/drug/PA165958378
Wikipedia
http://en.wikipedia.org/wiki/Gadofosveset
Drugs.com
http://www.drugs.com/mtm/gadofosveset-trisodium.html
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