Gadoteridol is a gadolinium-based contrast agent (GBCA) used with contrasted magnetic resonance imaging (MRI) to detect and visualize lesions and abnormal vascularity.

Brand Names
Generic Name
DrugBank Accession Number

Gadoteridol is a macrocyclic nonionic gadolinium that provides contrast enhancement of the brain, spine, and surrounding tissues, resulting in improved visualization (compared with unenhanced MRI) of lesions with abnormal vascularity or those thought to disrupt the normal blood-brain barrier.1,2,4 It was 1 of the 3 macrocyclic gadolinium-based contrast agents (GBCAs) that was mandated by the EMA to replace linear gadolinium-based contrast agents due to concerns about retained gadolinium in the brain.1

Initially approved by the FDA in 1992, gadoteridol received additional approval in 2020 for use in pediatric patients less than 2 years old.5

Small Molecule
Approved, Investigational
Average: 558.68
Monoisotopic: 559.127724835
Chemical Formula
  • gadolinium 2,2',2''-[10-(2-hydroxypropyl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl]triacetate
  • gadolinium-HP-DO3A
  • Gadoteridol
  • Gadoteridolum
  • GD-HP-DO 3A
  • Gd-HPDO3A
External IDs
  • Gd-HP-DO 3A
  • SQ 32692



Gadoteridol is indicated for use with magnetic resonance imaging (MRI) in order to visualize lesions with disrupted blood-brain barrier and/or abnormal vascularity in the brain, spine, and associated tissues in adult and pediatric patients, including term neonates.4 It is also indicated for visualization of lesions in the head and neck in adult patients.4

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Diagnostic agentCns abnormal vascularity•••••••••••••••••• ••••••••• ••••••••••••••••••
Diagnostic agentCentral nervous system lesion•••••••••••••••••• ••••••••• ••••••••••••••••••
Diagnostic agentLesions of the head and neck••••••••••••••••••••••••••
Contraindications & Blackbox Warnings
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Gadoteridol affects proton relaxation times and consequently the MR signal. Signal intensity is affected by the dose and relaxivity of the gadoteridol molecule. Consistently, for all gadolinium-based contrast agents, the relaxivity of gadoteridol decreases with the increase of the magnetic field strength used in clinical MRI (0.2 –3.0T).4

Disruption of the blood-brain barrier or abnormal vascularity allows the accumulation of gadoteridol in lesions such as neoplasms, abscesses, and subacute infarcts. The pharmacokinetics of gadoteridol in various lesions is not known.4

Mechanism of action

Gadoteridol is a paramagnetic agent and, as such, develops a magnetic moment when placed in a magnetic field. The relatively large magnetic moment produced by the paramagnetic agent results in a relatively large local magnetic field, which can enhance the relaxation rates of water protons in the vicinity of the paramagnetic agent.4

In MRI, visualization of normal and pathologic brain tissue depends, in part, on variations in the radiofrequency signal intensity that occur with: 1) differences in proton density; 2) differences of the spinlattice or longitudinal relaxation times (T1); and 3) differences in the spin-spin or transverse relaxation time (T2). When placed in a magnetic field, gadoteridol decreases T1 relaxation times in the target tissues. At recommended doses, the effect is observed with greatest sensitivity in the T1-weighted sequences.4


From population PK model of pediatric subjects receiving a single intravenous dose of 0.1 mmol/kg of gadoteridol, the mean Cmax was 0.66 ± 0.21 mmol/L in pediatric subjects 2 years to 6 years of age, 0.58 ± 0.06 mmol/L in pediatric subjects 6 years to 12 years of age, and 0.68 ± 0.12 mmol/L in adolescent subjects older than 12 years. The mean AUC0-∞ was 0.74 ± 0.20 mmol/Lh in pediatric subjects 2 years to 6 years of age, 0.74 ± 0.09 mmol/Lh in pediatric subjects 6 years to 12 years of age, and 0.98 ± 0.09 mmol/L*h in adolescent subjects older than 12 years of age. Pharmacokinetic simulations indicate similar half-life, AUC, and Cmax values for ProHance in pediatric subjects less than 2 years of age when compared to those reported for adults.4

Volume of distribution

The plasma distribution volume (mean ± SD) for the non-renally impaired adults was 0.205 ± 0.025 L/kg.Following GBCA administration, gadolinium is present for months or years in the brain, bone, skin, and other organs. 4

Protein binding

It is unknown if protein binding of gadoteridol occurs in vivo.4


It is unknown if biotransformation or decomposition of gadoteridol occurs in vivo.4

Route of elimination

Gadoteridol is eliminated in the urine with 94.4 ± 4.8% (mean ± SD) of the dose excreted within 24 hours post-injection. Over 80% of the dose was recovered in urine for pediatric subjects after 10 hours.4

In patients with moderately and severely impaired renal function about 97% and 76% of the administered dose was recovered in the urine within 7 days and 14 days, respectively.4


The elimination half-life (mean ± SD) is about 1.57 ± 0.08 hours.4

From population PK model of pediatric subjects receiving a single intravenous dose of 0.1 mmol/kg of gadoteridol, the mean distribution half-life (t1/2,alpha) was 0.14 ± 0.04 hours in pediatric subjects 2 years to 6 years of age, 0.18 ± 0.07 hours in pediatric subjects 6 years to 12 years of age, and 0.20 ± 0.07 hours in adolescent subjects older than 12 years of age. The mean elimination half-life (t1/2,beta) was 1.32 ± 0.006 hours in pediatric subjects 2 years to 6 years, 1.32 ± 0.07 hours in pediatric subjects 6 years to 12 years of age, and 1.61 ± 0.19 hours in adolescent subjects older than 12 years of age. Pharmacokinetic simulations indicate similar half-life values for gadoteridol in pediatric subjects less than 2 years of age when compared to those reported for adults.4

In patients with impaired renal function, the serum half-life of gadoteridol is prolonged. After intravenous injection of 0.1 mmol/kg, the elimination half-life of gadoteridol was 10.65 ± 0.06 hours in mild to moderately impaired patients (creatinine clearance 30 to 60 mL/min) and 9.10±0.26 hours in severely impaired patients not on dialysis (creatinine clearance 10 to 30 mL/min).4


The renal and plasma clearance rates (1.41 ± 0.33 mL/ min/kg and 1.50 ± 0.35 mL/ min/kg, respectively) of gadoteridol are essentially identical, indicating no alteration in elimination kinetics on passage through the kidneys and that the drug is essentially cleared through the kidney.4

The mean serum clearance of gadoteridol in patients with normal renal function was 116.14 ± 26.77 mL/min, compared to 37.2 ± 16.4 mL/min in patients with mild to moderate renal impairment and 16.0 ± 3.0 mL/min in patients with severe renal impairment.4

Adverse Effects
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Gadolinium-based contrast agents (GBCAs) cross the placenta and result in fetal exposure and gadolinium retention. The human data on the association between GBCAs and adverse fetal outcomes are limited and inconclusive. Because of the potential risks of gadolinium to the fetus, use gadoteridol only if imaging is essential during pregnancy and cannot be delayed.4

In animal reproduction studies in rats, gadoteridol doubled the incidence of post-implantation loss at up to 16 times the recommended human dose (RHD). There were no adverse developmental effects observed in rabbits with intravenous administration of gadoteridol during organogenesis at doses up to 19 times the recommended human dose of 0.1 mmol/kg.4

Clinical consequences of overdose with gadoteridol have not been reported. The safety of gadoteridol has been tested in clinical studies using doses up to 0.3 mmol/kg and no clinical consequences related to increasing dose have been observed to date. Gadoteridol can be removed by hemodialysis.4

No animal studies have been performed to evaluate the carcinogenic potential of gadoteridol.4

No changes in reproductive performance and outcome of pregnancy were caused in rats and rabbits by daily intravenous administration of gadoteridol to parent animals before and during gestation up to 1.5 mmol/kg/day (15 times the recommended human dose).4

Gadoteridol did not demonstrate genotoxic activity in: bacterial reverse mutation assays using Salmonella typhimurium and Escherichia coli; a mouse lymphoma forward mutation assay; an in vitro cytogenetic assay measuring chromosomal aberration frequencies in Chinese hamster ovary cells; and an in vivo mouse micronucleus assay at intravenous doses up to 5.0 mmol/kg.4

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.
AbacavirGadoteridol may decrease the excretion rate of Abacavir which could result in a higher serum level.
AceclofenacAceclofenac may decrease the excretion rate of Gadoteridol which could result in a higher serum level.
AcemetacinAcemetacin may decrease the excretion rate of Gadoteridol which could result in a higher serum level.
AcetaminophenAcetaminophen may decrease the excretion rate of Gadoteridol which could result in a higher serum level.
AcetazolamideAcetazolamide may increase the excretion rate of Gadoteridol which could result in a lower serum level and potentially a reduction in efficacy.
Food Interactions
No interactions found.


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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
ProHanceInjection, solution279.3 mg/1mLIntravenousBracco Diagnostics Inc2003-10-09Not applicableUS flag
ProHanceLiquid279.3 mg / mLIntravenousSquibb Diagnostics, Division Of Bristol Myers Squibb Canada Inc.1993-12-311998-07-30Canada flag
ProHanceInjection, solution279.3 mg/1mLIntravenousBIPSO GmbH1992-11-162016-11-09US flag
ProHanceSolution279.3 mg / mLIntravenousBracco Imaging S.P.A.1998-09-08Not applicableCanada flag


ATC Codes
V08CA04 — Gadoteridol
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 / Trialkylamines / Secondary alcohols / Carboxylic acid salts / Amino acids / 1,2-aminoalcohols / Carboxylic acids / Azacyclic compounds / Organopnictogen compounds / Organic zwitterions
show 4 more
1,2-aminoalcohol / Alcohol / Aliphatic heteromonocyclic compound / Alpha-amino acid / Amine / Amino acid / Azacycle / Carbonyl group / Carboxylic acid / Carboxylic acid salt
show 14 more
Molecular Framework
Aliphatic heteromonocyclic compounds
External Descriptors
gadolinium coordination entity (CHEBI:31643)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

CAS number
InChI Key
gadolinium(3+) 2-[4,7-bis(carboxylatomethyl)-10-(2-hydroxypropyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetate


General References
  1. Del Poggio A, Anello G, Calloni SF, Vezzulli P, Pereira C, Iadanza A, Falini A, Anzalone N: Diagnostic efficacy and safety of gadoteridol compared to gadobutrol and gadoteric acid in a large sample of CNS MRI studies at 1.5T. J Neuroradiol. 2022 Jan;49(1):73-79. doi: 10.1016/j.neurad.2020.06.005. Epub 2020 Jun 27. [Article]
  2. Gutierrez JE, Rosenberg M, Seemann J, Breuer J, Haverstock D, Agris J, Balzer T, Anzalone N: Safety and Efficacy of Gadobutrol for Contrast-enhanced Magnetic Resonance Imaging of the Central Nervous System: Results from a Multicenter, Double-blind, Randomized, Comparator Study. Magn Reson Insights. 2015 Apr 7;8:1-10. doi: 10.4137/MRI.S19794. eCollection 2015. [Article]
  3. FDA Approved Drug Products: Prohance (gadoteridol) injection for intravenous administration [Link]
  4. FDA Approved Drug Products: PROHANCE (gadoteridol injection) single dose, for intravenous use (Jan 2024) [Link]
  5. FDA Approves Bracco Diagnostics Inc.'s ProHance® (Gadoteridol) Injection, 279.3 mg/mL, for Pediatric Patients Younger than Two Years [Link]
Human Metabolome Database
PubChem Compound
PubChem Substance
FDA label
Download (195 KB)
Download (60.6 KB)

Clinical Trials

Clinical Trials
4CompletedDiagnosticBrain Disorders1
4CompletedDiagnosticCoronary Artery Disease (CAD) / Type 1 Diabetes Mellitus1
4RecruitingOtherCognitive Functioning / Contrast Medium / Motor Function1
3CompletedDiagnosticBrain Metastases1
3CompletedDiagnosticCentral Nervous System Disorder / Imaging procedure1


  • Bracco diagnostics inc
  • Bracco Diagnostics Inc.
  • Nycomed Inc.
Dosage Forms
Injection, solutionIntravenous279.3 mg/1mL
Injection, solutionIntravenous279.3 MG/ML
LiquidIntravenous279.3 mg / mL
SolutionIntravenous279.3 mg / mL
SolutionIntravenous279.3 mg
Injection, solutionParenteral
Unit descriptionCostUnit
Prohance 279.3 mg/ml vial6.81USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5474756No1995-12-122012-12-12US flag
CA1341176No2001-01-302018-01-30Canada flag
US5846519No1998-12-082015-12-08US flag


Experimental Properties
Not Available
Predicted Properties
Water Solubility11.2 mg/mLALOGPS
pKa (Strongest Acidic)1.46Chemaxon
pKa (Strongest Basic)8.3Chemaxon
Physiological Charge-2Chemaxon
Hydrogen Acceptor Count11Chemaxon
Hydrogen Donor Count1Chemaxon
Polar Surface Area153.58 Å2Chemaxon
Rotatable Bond Count8Chemaxon
Refractivity133.55 m3·mol-1Chemaxon
Polarizability39.38 Å3Chemaxon
Number of Rings1Chemaxon
Rule of FiveNoChemaxon
Ghose FilterNoChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
Human Intestinal Absorption-0.8097
Blood Brain Barrier+0.6442
Caco-2 permeable-0.5567
P-glycoprotein substrateSubstrate0.7825
P-glycoprotein inhibitor INon-inhibitor0.8295
P-glycoprotein inhibitor IINon-inhibitor0.8408
Renal organic cation transporterNon-inhibitor0.8026
CYP450 2C9 substrateNon-substrate0.8605
CYP450 2D6 substrateNon-substrate0.769
CYP450 3A4 substrateNon-substrate0.6437
CYP450 1A2 substrateNon-inhibitor0.8814
CYP450 2C9 inhibitorNon-inhibitor0.8843
CYP450 2D6 inhibitorNon-inhibitor0.8737
CYP450 2C19 inhibitorNon-inhibitor0.81
CYP450 3A4 inhibitorNon-inhibitor0.908
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9838
Ames testNon AMES toxic0.7586
BiodegradationNot ready biodegradable0.6054
Rat acute toxicity2.1688 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6113
hERG inhibition (predictor II)Non-inhibitor0.8966
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)


Mass Spec (NIST)
Not Available
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSsplash10-05mt-3009000000-8c8257add253983cc0f1
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
DarkChem Lite v0.1.0
DarkChem Lite v0.1.0
DarkChem Lite v0.1.0

Drug created at June 13, 2005 13:24 / Updated at May 03, 2024 10:01