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Gadofosveset Trisodium

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Also known as: Gadofosveset trisodium, 193901-90-5, Gadofosveset trisodium (usan), 211570-55-7, Ablavar (tn), Dtxsid501027793

Molecular Formula

C₃₃H₄₀GdN₃Na₃O₁₅P

Molecular Weight

975.9 g/mol

InChI Key

PIZALBORPSCYJU-UHFFFAOYSA-H

Gadofosveset Trisodium is the trisodium salt form of gadofosveset, an injectable, intravascular, amphiphilic gadolinium-based contrast agent (GBCA) used with magnetic resonance angiography (MRA) imaging. Gadofosveset is a stable gadolinium diethylenetriaminepentaacetic acid (Gd-DTPA) chelate derivative with a diphenylcyclohexylphosphate group. Upon injection, gadofosveset binds reversibly to endogenous serum albumin which increases its intravascular retention time compared to non-protein binding contrast agents. The serum albumin binding also increases T1-relaxivity of gadofosveset. This produces an increase in signal intensity of blood, thereby enhancing the visualization of blood vessels upon MRA and may aid in the diagnosis of certain blood vessels and heart disorders.

1 2D Structure

Gadofosveset Trisodium

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

trisodium;2-[[2-[bis(carboxylatomethyl)amino]-3-[(4,4-diphenylcyclohexyl)oxy-oxidophosphoryl]oxypropyl]-[2-[bis(carboxylatomethyl)amino]ethyl]amino]acetate;gadolinium(3+);hydrate

2.1.2 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

2.1.3 InChI Key

PIZALBORPSCYJU-UHFFFAOYSA-H

2.1.4 Canonical SMILES

C1CC(CCC1OP(=O)([O-])OCC(CN(CCN(CC(=O)[O-])CC(=O)[O-])CC(=O)[O-])N(CC(=O)[O-])CC(=O)[O-])(C2=CC=CC=C2)C3=CC=CC=C3.O.[Na+].[Na+].[Na+].[Gd+3]

2.2 Synonyms

2.2.1 MeSH Synonyms

1. Gadofosveset

2. Gadofosveset Trisodium

3. Ms 325

4. Ms-325

5. Vasovist

2.2.2 Depositor-Supplied Synonyms

1. Gadofosveset Trisodium

2. 193901-90-5

3. Gadofosveset Trisodium (usan)

4. 211570-55-7

5. Ablavar (tn)

6. Dtxsid501027793

7. D04286

8. Q5516411

9. Gadolinium Sodium 4-(bis(carboxylatomethyl)amino)-6,9-bis(carboxylatomethyl)-1-((4,4-diphenylcyclohexyl)oxy)-1-oxido-2-oxa-6,9-diaza-1-phosphaundecan-11-oate 1-oxide Hydrate (1:3:1:1)

2.3 Create Date

2008-02-08

3 Chemical and Physical Properties

Molecular Formula	C₃₃H₄₀GdN₃Na₃O₁₅P
Molecular Weight	975.9 g/mol
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	18
Rotatable Bond Count	18
Exact Mass	976.11312 g/mol
Monoisotopic Mass	976.11312 g/mol
Topological Polar Surface Area	270 Å²
Heavy Atom Count	56
Formal Charge	0
Complexity	1130
Isotope Atom Count	0
Defined Atom Stereocenter Count	0
Undefined Atom Stereocenter Count	1
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	6

4 Drug and Medication Information

4.1 Drug Information

1 of 2
Drug Name	Ablavar
PubMed Health	Gadofosveset (Injection)
Drug Classes	Diagnostic Agent, Radiological Contrast Media
Drug Label	ABLAVAR (gadofosveset trisodium) Injection is a sterile, nonpyrogenic, formulation of a stable gadolinium diethylenetriaminepentaacetic acid (GdDTPA) chelate derivative with a diphenylcyclohexylphosphate group. Each mL of ABLAVAR Injection contains 2...
Active Ingredient	Gadofosveset trisodium
Dosage Form	Solution
Route	Intravenous
Strength	3660mg/15ml (244mg/ml); 2440mg/10ml (244mg/ml)
Market Status	Prescription
Company	Lantheus Medcl

2 of 2
Drug Name	Ablavar
PubMed Health	Gadofosveset (Injection)
Drug Classes	Diagnostic Agent, Radiological Contrast Media
Drug Label	ABLAVAR (gadofosveset trisodium) Injection is a sterile, nonpyrogenic, formulation of a stable gadolinium diethylenetriaminepentaacetic acid (GdDTPA) chelate derivative with a diphenylcyclohexylphosphate group. Each mL of ABLAVAR Injection contains 2...
Active Ingredient	Gadofosveset trisodium
Dosage Form	Solution
Route	Intravenous
Strength	3660mg/15ml (244mg/ml); 2440mg/10ml (244mg/ml)
Market Status	Prescription
Company	Lantheus Medcl

4.2 Therapeutic Uses

Ablavar 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.

NIH; DailyMed. Current Medication Information for Ablavar-(gadofosveset trisodium injection, solution) (Updated: August 2013). Available from, as of March 13, 2015: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8175d0e7-b627-6c68-73e6-d1fc7660775d

4.3 Drug Warning

/BOXED WARNING/ WARNING: NEPHROGENIC SYSTEMIC FIBROSIS (NSF) Gadolinium-based contrast agents (GBCAs) increase the risk for NSF among patients with impaired elimination of the drugs. Avoid use of GBCAs in these patients unless the diagnostic information is essential and not available with non-contrasted MRI or other modalities. NSF may result in fatal or debilitating fibrosis affecting the skin, muscle and internal organs. The risk for NSF appears highest among patients with: chronic, severe kidney disease (GFR < 30 mL/min/1.73m sq), or acute kidney injury. Screen patients for acute kidney injury and other conditions that may reduce renal function. For patients at risk for chronically reduced renal function (e.g. age > 60 years, hypertension or diabetes), estimate the glomerular filtration rate (GFR) through laboratory testing. For patients at highest risk for NSF, do not exceed the recommended ABLAVAR dose and allow a sufficient period of time for elimination of the drug from the body prior to re-administration.

In patients with renal insufficiency, acute renal failure requiring dialysis or worsening renal function have occurred with the use of other gadolinium agents. The risk of renal failure may increase with increasing dose of gadolinium contrast. Screen all patients for renal dysfunction by obtaining a history and/or laboratory tests. Consider follow-up renal function assessments for patients with a history of renal dysfunction. No reports of acute renal failure were observed in clinical trials of ABLAVAR.

In clinical trials, a small increase (2.8 msec) in the average change from baseline in QTc was observed at 45 minutes following Ablavar administration; no increase was observed at 24 and 72 hours. A QTc change of 30 to 60 msec from baseline was observed in 39/702 (6%) patients at 45 min following Ablavar administration. At this time point, 3/702 (0.4%) patients experienced a QTc increase of > 60 msec. These QTc prolongations were not associated with arrhythmias or symptoms. In patients at high risk for arrhythmias due to QTc prolongation (e.g., concomitant medications, underlying cardiac conditions) consider obtaining baseline electrocardiograms to help assess the risks for Ablavar administration. If Ablavar is administered to these patients, consider follow-up electrocardiograms and risk reduction measures (e.g., patient counseling or intensive electrocardiography monitoring) until most Ablavar has been eliminated from the blood. In patients with normal renal function, most Ablavar was eliminated from the blood by 72 hours following injection.

Ablavar may cause anaphylactoid and/or anaphylactic reactions, including life-threatening or fatal reactions. In clinical trials, anaphylactoid and/or anaphylactic reactions occurred in two of 1676 subjects. If anaphylactic or anaphylactoid reactions occur, stop ABLAVAR Injection and immediately begin appropriate therapy. Observe patients closely, particularly those with a history of drug reactions, asthma, allergy or other hypersensitivity disorders, during and up to several hours after ablavar administration. Have trained personnel and emergency resuscitative equipment available prior to and during ablavar administration. If such a reaction occurs stop ablavar and immediately begin appropriate therapy.

For more Drug Warnings (Complete) data for Gadofosveset trisodium (9 total), please visit the HSDB record page.

4.4 Drug Indication

This medicinal product is for diagnostic use only.

Ablavar is indicated for contrast-enhanced magnetic resonance angiography (CE-MRA) for visualisation of abdominal or limb vessels in adults only, with suspected or known vascular disease.

5 Pharmacology and Biochemistry

5.1 MeSH Pharmacological Classification

Contrast Media

Substances used to allow enhanced visualization of tissues. (See all compounds classified as Contrast Media.)

5.2 ATC Code

V08CA

5.3 Absorption, Distribution and Excretion

Gadofosveset is eliminated primarily in the urine, with between 79% and 94% (mean of 83.7%) of an injected dose recovered in the urine. Of the total gadofosveset recovered in urine, 94% is recovered within the first 72 hours. A small portion of gadofosveset dose is recovered in feces (approximately 4.7%).

The mean volume of distribution at steady state for gadofosveset was 148 +/- 16 mL/kg, roughly equivalent to that of extracellular fluid. A significant portion of circulating gadofosveset is bound to plasma proteins, predominantly albumin. At 0.05, 0.5, 1 and 4 hours after injection of 0.03 mmol/kg the plasma protein binding of gadofosveset ranges from 79.8 to 87.4%.

The pharmacokinetics of intravenously administered gadofosveset conforms to a two-compartment open model with mean plasma concentrations (reported as mean +/-SD) of 0.43 +/- 0.04 mmol/L at 3 minutes post-injection, and 0.24 +/- 0.03 mmol/L at one hour post-injection. The mean half-life of the distribution phase is 0.48 +/- 0.11 hours and the mean half-life of the elimination phase is 16.3 +/- 2.6 hours. The mean total clearance of gadofosveset is 6.57 +/- 0.97 mL/h/kg following the administration of 0.03 mmol/kg.

In animal studies, less than 1% of gadofosveset at doses up to 0.3 mmol/kg was secreted in the milk of lactating rats.

5.4 Metabolism/Metabolites

Gadofosveset does not undergo measurable metabolism in humans.

5.5 Biological Half-Life

The mean half-life of the distribution phase is 0.48 +/- 0.11 hours and the mean half-life of the elimination phase is 16.3 +/- 2.6 hours.

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