Gadobutrol is a contrast agent used during diagnostic procedures to visualize disrupted areas of blood brain barrier (BBB) and/or abnormal vascularity of the central nervous system.

Brand Names
Gadavist, Gadovist
Generic Name
DrugBank Accession Number

Intravenous gadobutrol is a second-generation extracellular non-ionic macrocyclic GBCA (gadolinium-based contrast agent) used in magnetic resonance imaging (MRI) in adults and children older than 2 years of age. It may help visualize and detect vascular abnormalities in the blood brain barrier (BBB) and central nervous system (CNS).

In patients with impaired renal function, gadolinium based contrast agents increase the risk of nephrogenic systemic fibrosis (NSF). A physician should be contacted if symptoms of NSF are encountered, such as dark or red patches on the skin; stiffness in joints; trouble moving, bending or straightening arms, hands, legs or feet; burning, itching, swelling, scaling, hardening and tightening of skin; pain in hip bones or ribs; or muscle weakness.

Common adverse reactions that may be experienced include headache, nausea, feeling hot, abnormal taste, and warmth, burning or pain local to the injection site.

General precautions should be taken in patients who are pregnant or breastfeeding, or who have a history of allergic reaction to contrast media, bronchial asthma or an allergic respiratory disorder.

Small Molecule
Average: 604.72
Monoisotopic: 605.13321
Chemical Formula
  • Gadobutrol
  • gadolinium(III) 2,2',2''-(10-((2R,3S )-1,3,4-trihydroxybutan-2-yl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl)triacetate
External IDs
  • BAY86-4875
  • ZK-135079



Gadobutrol is indicated for use with magnetic resonance imaging for the following diagnostic processes:4

  • To detect and visualize areas with disrupted blood-brain barrier and/or abnormal vascularity of the central nervous system in adult and pediatric patients, including term neonates
  • To assess the presence and extent of malignant breast disease in adult patients
  • To evaluate known or suspected supra-aortic or renal artery disease in adult and pediatric patients, including term neonates
  • To assess myocardial perfusion (under stress and at rest) and late gadolinium enhancement in adult patients with known or suspected coronary artery disease
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Associated Conditions
Contraindications & Blackbox Warnings
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Even at low concentrations Gadobutrol can lead to distinct shortening of relaxation times of protons in plasma. At physiological conditions (pH=7, temperature=37°C), and 1.5T, the relaxivity (r1) is 5.2L/(mmol·sec) based on the relaxation times (T1), while the relativity (r2) is 6.1L/(mmol·sec) based on relaxation times (T2).

Magnetic field strength has only slight influence on relaxivities.

Drug concentration and r1 relaxivity may contribute to a T1 shortening effect, which may improve tissue visualization.

Mechanism of action

MRI tissue visualization is dependent, in part, on variations in intensity of radiofrequency signals which occur due to differences in proton density, differences of the spin-lattice or longitudinal relaxation times (T1), and differences in the spin-spin or transverse relaxation times (T2).

Gadolinium shortens T1 and T2 relaxation times. Greater signal enhancement is achieved with increased shortening of T1 and T2. The extent to which Gadolinium can shorten T1 and T2 is influenced by concentration in tissue, MRI field strength, and the relative ratio of transverse and longitudinal relaxation times.

The recommended dose produced the greatest sensitivity of T1 shortening effect in T1-weighted magnetic resonance sequences. In T2-weighted sequences, the large magnetic moment of gadolinium induced local magnetic field inhomogenenities.

At high concentrations used during bolus injections, T2-weighted sequences show a signal decrease.


With normal renal function, the AUC is 1.1 ± 0.1 mmol·h/L.

Volume of distribution

Rapid distribution to extracellular space occurs after intravenous administration.

After a dose of 0.1mmol/kg body weight, an average plasma level of 0.59 mmol/L was measured 2 minutes post injection, and 0.3mmol/L 60 minutes post injection.

Protein binding

No particular protein binding is displayed.


Gadobutrol is not metabolized.

Route of elimination

Excreted unchanged via glomerular filtration by the kidneys. Extrarenal elimination is negligible.


1.81 hours (1.33-2.13 hours).


In healthy subjects, renal clearance is 1.1 - 1.7mL/(min·kg). Within 2 hours of intravenous injection more than 50% is eliminated via the urine. Within 12 hours more than 90% of the given dose is eliminated.

Clearance was observed to be slightly lower in elderly subjects, when using a 0.1mmol/kg dose.

In the pediatric population, the median AUC, clearance and elimination half life was observed to be similar across the age range of 2-17, based on a population pharmacokinetic analysis of 130 pediatric subjects aged 2-17. In children aged 2-6 (n=45) the median AUC of gadobutrol was 0.8 mmol·h/L, the median clearance was 0.13L/hr/kg, and the median elimination half life was 1.75h. In children aged 7-11 (n=39) the median AUC of gadobutrol was 1.0 mmol·h/L, the median clearance was 0.1L/hr/kg, and the median elimination half life was 1.61h. In children aged 12-17 (n=46) the median AUC of gadobutrol was 1.2 mmol·h/L, the median clearance was 0.09 L/hr/kg, and the median elimination half life was 1.65h. Approximately 99% (median value) of the dose was recovered in the urine after 6 hours.

A prolonged serum half life of gadobutrol is correlated with a reduction in creatinine clearance. In patients with mild-moderate renal impairment (80>CLCR>30 mL/min) the elimination half life was 5.8 ± 2.4 hours, the AUC was 4.0 ± 1.8 mmol·h/L, and complete recovery from the urine is seen within 72 hours. In patients with severe renal impairment (CLCR<30 mL/min) the elimination half life was 17.6 ± 6.2 hours, the AUC was 11.5 ± 4.3 mmol·h/L, and complete recovery from the urine is seen within 5 days.
Physicians may consider the prompt initiation of hemodialysis following gadobutrol administration to aid elimination, in patients who are already receiving hemodialysis. After one dialysis session 68% of the initial dose is removed, after the second session 94%, and after the third session 98%.

Adverse Effects
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Lethality was observed in rodents after a single intravenous administration of 20 mmol/kg. This represents a dose of at least 2 orders of magnitude higher than the standard single diagnostic dose in humans (0.1 mmol/kg).

No carcinogenicity studies have been conducted.

No mutagenesis was observed in vitro in reverse mutation tests in bacteria, or in the HGPRT (hypoxanthine-guanine phosphoribosyl transferase) test using Chinese hamster V79 cells. Similarly, no mutagenesis was seen in chromosome abberation tests of human peripheral blood lymphocytes. It was also negative in in-vivo micronucleus tests in mice following a 0.5mmol/kg intravenous injection.

No fertility or reproductive impairment was observed in male and female rates given doses 12.2 times human equivalent doses, based on body surface area.

Intolerance reactions local to the injection site have been observed in rabbits after paravenous administration, and are associated with the infiltration of inflammatory cells, suggesting the possibility of local irritation if the contrast medium leaks around veins in a clinical setting.

Not Available
Pharmacogenomic Effects/ADRs
Not Available


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.
No interactions found.
Food Interactions
  • Take with or without food.


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Active Moieties
Gadolinium cation (3+)ionicAZV954TZ9N22541-19-1RJOJUSXNYCILHH-UHFFFAOYSA-N
International/Other Brands
Gadovist (Bayer Schering Pharma)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
GadavistInjection604.72 mg/1mLIntravenousBayer HealthCare Pharmaceuticals Inc.2011-03-14Not applicableUS flag
Gadovist 1.0Solution604.72 mg / mLIntravenousBayer2004-01-30Not applicableCanada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
GadobutrolInjection604.72 mg/1mLIntravenousSlate Run Pharmaceuticals, Llc2023-10-20Not applicableUS flag
GadobutrolInjection604.72 mg/1mLIntravenousSlate Run Pharmaceuticals, Llc2023-06-01Not applicableUS flag
GadobutrolInjection604.72 mg/1mLIntravenousFresenius Kabi USA, LLC2023-10-01Not applicableUS flag
GadobutrolInjection604.72 mg/1mLIntravenousFresenius Kabi USA, LLC2023-04-14Not applicableUS flag
GadobutrolInjection604.72 mg/1mLIntravenousSlate Run Pharmaceuticals, Llc2023-10-20Not applicableUS flag
GadobutrolInjection604.72 mg/1mLIntravenousFresenius Kabi USA, LLC2023-10-01Not applicableUS flag


ATC Codes
V08CA09 — Gadobutrol
Drug Categories
Chemical TaxonomyProvided by Classyfire
This compound belongs to the class of organic compounds known as alpha amino acids. These are amino acids in which the amino group is attached to the carbon atom immediately adjacent to the carboxylate group (alpha carbon).
Organic compounds
Super Class
Organic acids and derivatives
Carboxylic acids and derivatives
Sub Class
Amino acids, peptides, and analogues
Direct Parent
Alpha amino acids
Alternative Parents
Tricarboxylic acids and derivatives / 1,3-aminoalcohols / Trialkylamines / Secondary alcohols / 1,2-aminoalcohols / Amino acids / Carboxylic acid salts / Polyols / Azacyclic compounds / Carboxylic acids
show 7 more
1,2-aminoalcohol / 1,3-aminoalcohol / Alcohol / Aliphatic heteromonocyclic compound / Alpha-amino acid / Amine / Amino acid / Azacycle / Carbonyl group / Carboxylic acid
show 17 more
Molecular Framework
Aliphatic heteromonocyclic compounds
External Descriptors
gadolinium coordination entity (CHEBI:68841)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

CAS number
InChI Key


Synthesis Reference

Orlin Petrov, Peter Blaszkiewicz, "Process for mono- and 1,7-bis-N-.beta.-hydroxyalkylation of cyclene; N-.beta.-hydroxyalkyl-1,4,7,10-tetraazacyclododecane-lithium-salt complexes and the use of the complexes for the production of gadobutrol and analogs." U.S. Patent US5994536, issued May, 1998.

General References
  1. Scott LJ: Gadobutrol: a review of its use for contrast-enhanced magnetic resonance imaging in adults and children. Clin Drug Investig. 2013 Apr;33(4):303-14. doi: 10.1007/s40261-013-0066-0. [Article]
  2. Wack C, Steger-Hartmann T, Mylecraine L, Hofmeister R: Toxicological safety evaluation of gadobutrol. Invest Radiol. 2012 Nov;47(11):611-23. doi: 10.1097/RLI.0b013e318263f128. [Article]
  3. Kunnemeyer J, Terborg L, Nowak S, Scheffer A, Telgmann L, Tokmak F, Gunsel A, Wiesmuller G, Reichelt S, Karst U: Speciation analysis of gadolinium-based MRI contrast agents in blood plasma by hydrophilic interaction chromatography/electrospray mass spectrometry. Anal Chem. 2008 Nov 1;80(21):8163-70. doi: 10.1021/ac801264j. Epub 2008 Sep 27. [Article]
  4. FDA Approved Drug Products: Gadavist (gadobutrol) injection for intravenous administration [Link]
Human Metabolome Database
PubChem Compound
PubChem Substance
RxList Drug Page Drug Page
FDA label
Download (103 KB)
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Clinical Trials

Clinical Trials
4CompletedDiagnosticBrain Disorders1
4CompletedDiagnosticBrain Lesions1
4CompletedDiagnosticMagnetic Resonance Imaging (MRI)1
4CompletedDiagnosticNeoplastic CNS Lesions1
4CompletedDiagnosticPeripheral Arterial Disease (PAD)1
4CompletedDiagnosticPrimary Brain Neoplasm1
4CompletedTreatmentFibrosis / Impaired Renal Function1
4RecruitingDiagnosticBreast Diseases1
4RecruitingDiagnosticImage, Body1
4RecruitingOtherCognitive Functioning / Contrast Medium / Motor Function1


Not Available
Not Available
Dosage Forms
InjectionIntravenous604.72 mg/1mL
Injection, solutionParenteral
Injection, solution
InjectionIntravenous0.5 MMOL/ML
InjectionIntravenous1 MMOL/ML
Injection, solutionIntravenous0.5 MMOL/ML
Injection, solutionIntravenous1 MMOL/ML
Injection, solutionParenteral1 MMOL/ML
Injection, solutionParenteral1.0 MMOL/ML
SolutionIntravenous604.72 mg/1ml
SolutionIntravenous604.72 mg / mL
SolutionIntravenous604.72 mg/ml
Injection, solutionIntravenous
InjectionIntravenous604.72 mg
InjectionIntravenous604.720 mg
SolutionIntravenous1 mmol
Not Available
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5980864No1999-11-092016-11-09US flag


Experimental Properties
Not Available
Predicted Properties
Water Solubility0.0496 mg/mLALOGPS
pKa (Strongest Acidic)0.99Chemaxon
pKa (Strongest Basic)-3Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count9Chemaxon
Hydrogen Donor Count3Chemaxon
Polar Surface Area181.08 Å2Chemaxon
Rotatable Bond Count10Chemaxon
Refractivity143.47 m3·mol-1Chemaxon
Polarizability45.39 Å3Chemaxon
Number of Rings4Chemaxon
Rule of FiveNoChemaxon
Ghose FilterNoChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleYesChemaxon
Predicted ADMET Features
Human Intestinal Absorption-0.9703
Blood Brain Barrier-0.7581
Caco-2 permeable-0.7342
P-glycoprotein substrateSubstrate0.7464
P-glycoprotein inhibitor INon-inhibitor0.9204
P-glycoprotein inhibitor IINon-inhibitor0.9222
Renal organic cation transporterNon-inhibitor0.8783
CYP450 2C9 substrateNon-substrate0.9002
CYP450 2D6 substrateNon-substrate0.8025
CYP450 3A4 substrateNon-substrate0.731
CYP450 1A2 substrateNon-inhibitor0.8461
CYP450 2C9 inhibitorNon-inhibitor0.8755
CYP450 2D6 inhibitorNon-inhibitor0.9271
CYP450 2C19 inhibitorNon-inhibitor0.8538
CYP450 3A4 inhibitorNon-inhibitor0.8888
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9958
Ames testNon AMES toxic0.6773
BiodegradationNot ready biodegradable0.561
Rat acute toxicity2.2102 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8805
hERG inhibition (predictor II)Non-inhibitor0.7963
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)


Mass Spec (NIST)
Download (21.2 KB)
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available

Drug created at May 15, 2010 17:36 / Updated at December 02, 2023 06:46