Tìm theo
Gadoxetate
Các tên gọi khác (2) :
  • Gd-EOB-DTPA
  • SHL-569B
contrast media, diagnostic agents
Thuốc Gốc
Small Molecule
CAS: 135326-22-6
ATC: V08CA10
CTHH: C23H28GdN3Na2O11
PTK: 725.71
Gadoxetate is a paramagnetic gadolinium-containing contrast agent in which its salt form, gadoxetate disodium, is used for intravenous injection. Ethoxybenzyl diethylenetriaminepentaacetic acid is the moiety that chelates with a gadolinium ion and forms a stable complex with it to make up the drug. It is marketed by Bayer HealthCare Pharmaceuticals and FDA approved on July 3, 2008.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C23H28GdN3Na2O11
Phân tử khối
725.71
Monoisotopic mass
726.076023636
InChI
InChI=1/C23H33N3O11.Gd.2Na/c1-2-37-18-5-3-16(4-6-18)9-17(26(14-22(33)34)15-23(35)36)10-24(11-19(27)28)7-8-25(12-20(29)30)13-21(31)32;;;/h3-6,17H,2,7-15H2,1H3,(H,27,28)(H,29,30)(H,31,32)(H,33,34)(H,35,36);;;/q;+3;2*+1/p-5
InChI Key
InChIKey=SLYTULCOCGSBBJ-UHFFFAOYNA-I
IUPAC Name
gadolinium(3+) ion disodium 2-({2-[bis(carboxylatomethyl)amino]-3-(4-ethoxyphenyl)propyl}({2-[bis(carboxylatomethyl)amino]ethyl})amino)acetate
Traditional IUPAC Name
gadolinium(3+) ion disodium 2-({2-[bis(carboxylatomethyl)amino]-3-(4-ethoxyphenyl)propyl}({2-[bis(carboxylatomethyl)amino]ethyl})amino)acetate
SMILES
[Na+].[Na+].[Gd+3].CCOC1=CC=C(CC(CN(CCN(CC([O-])=O)CC([O-])=O)CC([O-])=O)N(CC([O-])=O)CC([O-])=O)C=C1
Độ hòa tan
4.06e-01 g/l
logP
-4.3
logS
-3.3
pKa (strongest acidic)
1.98
pKa (Strongest Basic)
9.99
PSA
219.6 Å2
Refractivity
180.88 m3·mol-1
Polarizability
49.99 Å3
Rotatable Bond Count
20
H Bond Acceptor Count
14
H Bond Donor Count
0
Physiological Charge
-3
Number of Rings
1
Bioavailability
0
pKa
6.8-8
Dược Lực Học : Gadoxetate disodium is an amphipathic compound in which gadoxetate is hydrophillic and its moiety, the ethoxybenyzl group, is lipophillic. Consequently, gadoxetate disodium has a biphasic mode of action in which it first distributes into the extracellular space after bolus injection and then hepatocytes selectively takes up the drug.
Cơ Chế Tác Dụng : Gadoxetate is a paramagnetic gadolinium-containing contrast agent in which its salt form, gadoxetate disodium, is used for intravenous injection. Ethoxybenzyl diethylenetriaminepentaacetic acid is the moiety that chelates with a gadolinium ion and forms a stable complex with it to make up the drug. It is marketed by Bayer HealthCare Pharmaceuticals and FDA approved on July 3, 2008. When gadoxetate disodium is placed in an external magnetic field, a large magnetic moment is produced. As a result, a magnetic field is induced around the tissue. The water protons in the vicinity are disrupted such that the change the proton density and spin characteristics are detected and visualized by a device.
Dược Động Học :

▧ Volume of Distribution :
Total volume of distribution at steady state is 0.21 L/kg. Gadoxetate disodium cannot diffuse through the blood brain barrier. The two transporters that gadoxetate disodium can enter the hepatocyte through are OATP1B1 and OATP1B3. Gadoxetate disodium may also exit the heptaocyte and go back into sinusoidal space via active transport through multidrug resistance protein 3 and 4.
▧ Protein binding :
<10% protein bound. Because it is more protein bound than other gadolinium-based contrast agents, gadoxetate disodium has increased T1 relaxivity. This results in an enhancement of the signal.
▧ Metabolism :
Gadoxetate disodium is not metabolized.
▧ Route of Elimination :
Gadoxetate disodium is eliminated equally via urine and feces. Multidrug resistance protein 2 actively transports/excretes gadoxetate disodium into the bile.
▧ Half Life :
Terminal elimination half-life, healthy subjects, adults = 0.91 - 0.95 hours
▧ Clearance :
Clearance may be lower in older patients. Total serum clearance (CLtot) = 250 mL/min; Renal clearance (CLr) = 120 mL/min
Độc Tính : LD50, oral, rat = 18100 mg/kg; LD50, oral, mouse = 14500 mg/kg; LD50, IV, rat = 3600 - 7300 mg/kg; LD50, IV, mouse = 5400 - 10900 mg/kg; LD50, IV, dog = >2200 mg/kg
Chỉ Định : Gadoxetate is used as a contrast medium for magnetic resonance imaging (MRI) to detect and characterize lesions in the liver.
Tương Tác Thuốc :
  • Rifampicin Substrates of OATP1B1 and OATP1B3 may limit uptake of gadoxetate disodium into heptatocytes. This may alter the intensity of the signal.
Liều Lượng & Cách Dùng : Injection, solution - Intravenous - 0.25 mol/L
Dữ Kiện Thương Mại
Nhà Sản Xuất
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08884
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D04288
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/50419-320-05
PharmGKB
http://www.pharmgkb.org/drug/PA165985534
Wikipedia
http://en.wikipedia.org/wiki/Gadoxetic_acid
RxList
http://www.rxlist.com/eovist-drug.htm
Drugs.com
http://www.drugs.com/mtm/gadoxetate.html
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