Identification
- Summary
Gadofosveset trisodium is an intravenous contrast agent used during magnetic resonance angiography (MRA) to evaluate aortoiliac occlusive disease (AIOD) in adults with peripheral vascular disease.
- Brand Names
- Vasovist
- Generic Name
- Gadofosveset trisodium
- DrugBank Accession Number
- DB06705
- Background
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.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Gadofosveset trisodium (DB06705)
- Weight
- Average: 1003.85
Monoisotopic: 1004.081 - Chemical Formula
- C33H38GdN3Na5O14P
- Synonyms
- Gadofosveset
- External IDs
- MS-325
Pharmacology
- Indication
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.
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- Contraindications & Blackbox Warnings
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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.
- Mechanism of action
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.
- Absorption
Not Available
- 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.
- Adverse Effects
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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).
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Abacavir may decrease the excretion rate of Gadofosveset trisodium which could result in a higher serum level. Aceclofenac Aceclofenac may decrease the excretion rate of Gadofosveset trisodium which could result in a higher serum level. Acemetacin Acemetacin may decrease the excretion rate of Gadofosveset trisodium which could result in a higher serum level. Acetaminophen Acetaminophen may decrease the excretion rate of Gadofosveset trisodium which could result in a higher serum level. Acetazolamide Acetazolamide may increase the excretion rate of Gadofosveset trisodium which could result in a lower serum level and potentially a reduction in efficacy. Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Gadofosveset trisodium which could result in a higher serum level. Aclidinium Gadofosveset trisodium may decrease the excretion rate of Aclidinium which could result in a higher serum level. Acrivastine Gadofosveset trisodium may decrease the excretion rate of Acrivastine which could result in a higher serum level. Acyclovir Acyclovir may decrease the excretion rate of Gadofosveset trisodium which could result in a higher serum level. Adefovir dipivoxil Adefovir dipivoxil may decrease the excretion rate of Gadofosveset trisodium which could result in a higher serum level. 
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- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Gadofosveset trisodium monohydrate XM33Q67UVH 211570-55-7 PIZALBORPSCYJU-QSQMUHTISA-H - Active Moieties
Name Kind UNII CAS InChI Key Gadolinium cation (3+) ionic AZV954TZ9N 22541-19-1 RJOJUSXNYCILHH-UHFFFAOYSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ablavar Injection, solution 0.25 mmol/ml Intravenous Tmc Pharma Services Ltd. 2016-09-20 2011-11-14 EU 
Ablavar Injection, solution 0.25 mmol/ml Intravenous Tmc Pharma Services Ltd. 2016-09-20 2011-11-14 EU Ablavar Injection, solution 0.25 mmol/ml Intravenous Tmc Pharma Services Ltd. 2016-09-20 2011-11-14 EU Ablavar Injection, solution 0.25 mmol/ml Intravenous Tmc Pharma Services Ltd. 2016-09-20 2011-11-14 EU Ablavar Injection, solution 0.25 mmol/ml Intravenous Tmc Pharma Services Ltd. 2016-09-20 2011-11-14 EU Ablavar Injection, solution 0.25 mmol/ml Intravenous Tmc Pharma Services Ltd. 2016-09-20 2011-11-14 EU Ablavar Solution 244 mg / mL Intravenous Lantheus Mi Canada Inc 2010-10-12 2016-03-07 Canada 
Ablavar Injection, solution 0.25 mmol/ml Intravenous Tmc Pharma Services Ltd. 2016-09-20 2011-11-14 EU Ablavar Injection, solution 244 mg/1mL Intravenous Lantheus Medical Imaging 2008-12-12 2016-09-01 US 
Ablavar Injection, solution 0.25 mmol/ml Intravenous Tmc Pharma Services Ltd. 2016-09-20 2011-11-14 EU
Categories
- ATC Codes
- V08CA11 — Gadofosveset
- Drug Categories
- Compounds used in a research, industrial, or household setting
- Contrast Media
- Diagnostic Uses of Chemicals
- Drugs that are Mainly Renally Excreted
- Elements
- Gadolinium-based Contrast Agent
- Lanthanoid Series Elements
- Magnetic Resonance Angiography
- Magnetic Resonance Contrast Activity
- Magnetic Resonance Imaging Contrast Media
- Metals
- Metals, Rare Earth
- Paramagnetic Contrast Agent
- Paramagnetic Contrast Media
- Classification
- Not classified
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 9430ZR8ZAN
- CAS number
- 193901-90-5
- InChI Key
- XGOSYNSWSRUASG-SSMZTGFVSA-H
- InChI
- InChI=1S/C33H44N3O14P.Gd.3Na/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);;;;/q;+3;3*+1/p-6/t26-;;;;/m1..../s1
- IUPAC Name
- SMILES
- [Na+].[Na+].[Na+].[Gd+3].[O-]C(=O)CN(CCN(CC([O-])=O)CC([O-])=O)C[C@H](COP([O-])(=O)OC1CCC(CC1)(C1=CC=CC=C1)C1=CC=CC=C1)N(CC([O-])=O)CC([O-])=O
References
- General References
- Raman FS, Nacif MS, Cater G, Gai N, Jones J, Li D, Sibley CT, Liu S, Bluemke DA: 3.0-T whole-heart coronary magnetic resonance angiography: comparison of gadobenate dimeglumine and gadofosveset trisodium. Int J Cardiovasc Imaging. 2013 Jun;29(5):1085-94. doi: 10.1007/s10554-013-0192-z. Epub 2013 Mar 21. [Article]
- Hrdina L, Kocher M, Herman M, Cerna M, Kozak J, Tudos Z, Mahathmakanthi S, Langova K: Comparison of the quality of lower limb magnetic resonance angiographies performed with different paramagnetic contrast agents in relation to body mass index and ejection fraction. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2012 Jun;156(2):164-70. doi: 10.5507/bp.2011.058. [Article]
- Thouet T, Schnackenburg B, Kokocinski T, Fleck E, Nagel E, Kelle S: Visualization of chronic myocardial infarction using the intravascular contrast agent MS-325 (gadofosveset) in patients. ScientificWorldJournal. 2012;2012:236401. doi: 10.1100/2012/236401. Epub 2012 Mar 12. [Article]
- Milot L, Haider M, Foster L, McGregor C, Law C: Gadofosveset trisodium in the investigation of focal liver lesions in noncirrhotic liver: Early experience. J Magn Reson Imaging. 2012 Sep;36(3):738-42. doi: 10.1002/jmri.23650. Epub 2012 Apr 5. [Article]
- Caravan P: Protein-targeted gadolinium-based magnetic resonance imaging (MRI) contrast agents: design and mechanism of action. Acc Chem Res. 2009 Jul 21;42(7):851-62. doi: 10.1021/ar800220p. [Article]
- FDA Approved Drug Products: ABLAVAR (gadofosveset trisodium) injection [Link]
- External Links
- KEGG Drug
- D04286
- PubChem Compound
- 73049652
- PubChem Substance
- 175427086
- ChemSpider
- 9847191
- 1364289
- ChEMBL
- CHEMBL1908362
- PharmGKB
- PA165958378
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Gadofosveset
- FDA label
- Download (148 KB)
- MSDS
- Download (66.5 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Diagnostic Chronic Liver Diseases (CLD) 1 4 Completed Other Pediatric Congenital Heart Disease 1 4 Unknown Status Diagnostic Congenital Heart Disease (CHD) 1 4 Withdrawn Diagnostic Ovarian Neoplasms 1 3 Completed Diagnostic Peripheral Vascular Disease Patient 1 3 Completed Diagnostic Steno-Occlusive Disease 1 2 Completed Diagnostic Cancer 1 2 Completed Diagnostic Myocardial Ischemia 1 1 Completed Diagnostic Atherosclerosis / Chronic Total Aterial Occlusion / Intermittent Claudication / Peripheral Arterial Disease (PAD) 1 Not Available Completed Not Available Magnetic Resonance Imaging (MRI) / Neoplasms Staging / Rectal Neoplasms 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, solution Intravenous 0.25 mmol/ml Injection, solution Intravenous 244 mg/1mL Injection Intravenous 244 mg/1mL Injection, solution Intravenous Solution Intravenous 244 mg / mL - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA2304461 No 2008-10-14 2018-08-17 Canada CA2211100 No 2007-03-20 2016-01-16 Canada US6676929 No 2004-01-13 2020-05-04 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.169 mg/mL ALOGPS logP 3.84 ALOGPS logS -3.8 ALOGPS Rule of Five No Chemaxon Ghose Filter No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption - 0.8572 Blood Brain Barrier + 0.6355 Caco-2 permeable - 0.5948 P-glycoprotein substrate Substrate 0.6107 P-glycoprotein inhibitor I Inhibitor 0.6422 P-glycoprotein inhibitor II Non-inhibitor 0.6901 Renal organic cation transporter Non-inhibitor 0.6739 CYP450 2C9 substrate Non-substrate 0.7903 CYP450 2D6 substrate Non-substrate 0.8158 CYP450 3A4 substrate Non-substrate 0.5501 CYP450 1A2 substrate Non-inhibitor 0.7768 CYP450 2C9 inhibitor Non-inhibitor 0.7121 CYP450 2D6 inhibitor Non-inhibitor 0.8278 CYP450 2C19 inhibitor Non-inhibitor 0.6916 CYP450 3A4 inhibitor Non-inhibitor 0.7875 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8798 Ames test Non AMES toxic 0.6081 Carcinogenicity Non-carcinogens 0.7542 Biodegradation Not ready biodegradable 0.9604 Rat acute toxicity 2.6392 LD50, mol/kg Not applicable hERG inhibition (predictor I) Strong inhibitor 0.5557 hERG inhibition (predictor II) Non-inhibitor 0.5302
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
References
- Meaney JF, Goyen M: Recent advances in contrast-enhanced magnetic resonance angiography. Eur Radiol. 2007 Mar;17 Suppl 2:B2-6. [Article]
- Caravan P: Protein-targeted gadolinium-based magnetic resonance imaging (MRI) contrast agents: design and mechanism of action. Acc Chem Res. 2009 Jul 21;42(7):851-62. doi: 10.1021/ar800220p. [Article]
- Caravan P, Parigi G, Chasse JM, Cloutier NJ, Ellison JJ, Lauffer RB, Luchinat C, McDermid SA, Spiller M, McMurry TJ: Albumin binding, relaxivity, and water exchange kinetics of the diastereoisomers of MS-325, a gadolinium(III)-based magnetic resonance angiography contrast agent. Inorg Chem. 2007 Aug 6;46(16):6632-9. Epub 2007 Jul 11. [Article]
- Henness S, Keating GM: Gadofosveset. Drugs. 2006;66(6):851-7. [Article]
Drug created at May 16, 2010 00:37 / Updated at September 09, 2021 09:05