Details
Stereochemistry | RACEMIC |
Molecular Formula | C17H29N4O7.Gd |
Molecular Weight | 558.68 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[Gd+3].CC(O)CN1CCN(CC([O-])=O)CCN(CC([O-])=O)CCN(CC([O-])=O)CC1
InChI
InChIKey=DPNNNPAKRZOSMO-UHFFFAOYSA-K
InChI=1S/C17H32N4O7.Gd/c1-14(22)10-18-2-4-19(11-15(23)24)6-8-21(13-17(27)28)9-7-20(5-3-18)12-16(25)26;/h14,22H,2-13H2,1H3,(H,23,24)(H,25,26)(H,27,28);/q;+3/p-3
DescriptionCurator's Comment: description was created based on several sources, including:
http://www.drugbank.ca/drugs/DB00597
Curator's Comment: description was created based on several sources, including:
http://www.drugbank.ca/drugs/DB00597
Gadoteridol (INN) is a gadolinium-based MRI contrast agent, used particularly in the imaging of the central nervous system. It is sold under the brand name ProHance. 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. In magnetic resonance imaging (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 spin-lattice 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. Gadoteridol does not cross the intact blood-brain barrier and, therefore, does not accumulate in normal brain or in lesions that have a normal blood-brain barrier, e.g., cysts, mature post-operative scars, etc. However, disruption of the blood-brain barrier or abnormal vascularity allows accumulation of gadoteridol in lesions such as neoplasms, abscesses, and subacute infarcts. The pharmacokinetics of ProHance in various lesions is not known.
Approval Year
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Diagnostic | PROHANCE Approved UseGadoteridol Injection is indicated for use in MRI in adults and children over 2 years of age to visualize lesions with abnormal vascularity in the brain (intracranial lesions), spine and associated tissues. Launch Date1993 |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1.57 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1506147/ |
0.3 mmol/kg single, intravenous dose: 0.3 mmol/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
GADOTERIDOL serum | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
0.3 mmol/kg 1 times / day single, intravenous Highest studied dose Dose: 0.3 mmol/kg, 1 times / day Route: intravenous Route: single Dose: 0.3 mmol/kg, 1 times / day Sources: |
unknown, 56.7 (6 - 93) n = 6163 Health Status: unknown Age Group: 56.7 (6 - 93) Sex: M+F Population Size: 6163 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/201277Orig1s000PharmR.pdf#page=53 Page: 53.0 |
Sample Use Guides
ADULTS: The recommended dose of (Gadoteridol) Injection is 0.1 mmol/kg (0.2mL/kg) administered as a rapid intravenous infusion (10 mL/min-60 mL/min) or bolus ( >60 mL/min).
CHILDREN (2-18 years): The recommended dose is 0.1 mmol/kg (0.2mL/kg)
administered as a rapid intravenous infusion (10 mL/min-60 mL/min) or bolus (> 60 mL/min).
Route of Administration:
Intravenous
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Classification Tree | Code System | Code | ||
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NDF-RT |
N0000175862
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NDF-RT |
N0000180184
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WHO-ATC |
V08CA04
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NCI_THESAURUS |
C62358
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WHO-VATC |
QV08CA04
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GADOTERIDOL
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1268
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120066-54-8
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C062402
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6655
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60714
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31643
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DB00597
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CHEMBL1200593
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760055
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25483
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BB-97
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100000084509
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SUB07866MIG
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m5628
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Gadoteridol
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7549
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DTXSID2048662
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1287631
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0199MV609F
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0199MV609F
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C65796
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ACTIVE MOIETY