Indium In-111 pentetate

Identification

Summary

Indium In-111 pentetate is a radiopharmaceutical diagnostic agent used for radionuclide cisternography.

Brand Names
Indium DTPA In 111
Generic Name
Indium In-111 pentetate
DrugBank Accession Number
DB09425
Background

Indium In-111 pentetate disodium is a radioactive diagnostic indicated for use in radionuclide cisternography. Decay of In-111 by electron capture allows for detection with a gamma camera for visualization of the brain and spinal column.

Type
Small Molecule
Groups
Approved
Structure
Thumb
Weight
Average: 501.23
Monoisotopic: 501.019979533
Chemical Formula
C14H20InN3O10
Synonyms
  • Indium (111In) pentetic acid
  • Indium In 111 pentetate
  • Indium In-111 pentetate

Pharmacology

Indication

Pentetate Indium Disodium In 111 is recommended for use in radionuclide cisternography.

Pharmacology
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Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Not Available

Mechanism of action

Decay of In-111 by electron capture allows for detection with a gamma camera for visualization of the brain and spinal column.

Absorption

After intrathecal administration, the radiopharmaceutical is absorbed from the subarachnoid space as described below, and the remainder flows superiorly to the basal cisterns within 2 to 4 hours and subsequently will be apparent in the Sylvian cisterns, the interhemispheric cisterns, and over the cerebral convexities. In normal individuals, the radiopharmaceutical will have ascended to the parasagittal region within 24 hours with simultaneous partial or complete clearance of activity from the basal cisterns and Sylvian regions. In contrast to air, the radiopharmaceutical does not normally enter the cerebral ventricles. Although the primary absorption of cerebrospinal fluid (CSF) into the blood stream occurs at the arachnoid villi, there is some evidence that a significant fraction of CSF is also absorbed across both the cerebral and spinal leptomeninges. Lesser quantities may also be absorbed across the ventricular ependyma. It is also generally held that these alternate routes of CSF absorption may assume primary importance when the major routes of the flow are pathologically obstructed

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Approximately 65% of the administered dose is excreted by the kidneys within 24 hours and this increases to 85% in 72 hours.

Half-life

Indium 111 decays by electron capture with a physical half-life of 67.9 hours.

Clearance

Not Available

Adverse Effects
Adverseeffects
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Toxicity

Pregnancy Category C

Aseptic meningitis and pyrogenic reactions have been rarely (less than 0.4%) observed following cisternography

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.
Not Available
Food Interactions
No interactions found.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Indium In-111 pentetate disodium7UIT3ZGC8E60662-14-8JKGXLBAWNSPIFF-LWQDMHIUSA-I
Active Moieties
NameKindUNIICASInChI Key
Pentetic acidunknown7A314HQM0I67-43-6QPCDCPDFJACHGM-UHFFFAOYSA-N
Indium cation In-111ionicWJZ06C0H8L131391-70-3RJMMFJHMVBOLGY-AHCXROLUSA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
In-111 DTPASolution3.75 mCi/1.5mLIntrathecalAnazao Health Corporation2012-06-19Not applicableUS flag
Indium DTPA In 111Solution1 mCi/1mLIntrathecalMedi-Physics, Inc. dba GE Healthcare1982-02-18Not applicableUS flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
In-111 DTPAIndium In-111 pentetate disodium (3.75 mCi/1.5mL)SolutionIntrathecalAnazao Health Corporation2012-06-19Not applicableUS flag

Categories

ATC Codes
V09AX01 — Indium (111in) pentetic acid
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as pentacarboxylic acids and derivatives. These are carboxylic acids containing exactly five carboxyl groups.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
Carboxylic acids and derivatives
Sub Class
Pentacarboxylic acids and derivatives
Direct Parent
Pentacarboxylic acids and derivatives
Alternative Parents
Alpha amino acids / Trialkylamines / Carboxylic acid salts / Amino acids / Carboxylic acids / Organic zwitterions / Organic salts / Organic oxides / Hydrocarbon derivatives / Carbonyl compounds
Substituents
Aliphatic acyclic compound / Alpha-amino acid / Alpha-amino acid or derivatives / Amine / Amino acid / Amino acid or derivatives / Carbonyl group / Carboxylic acid / Carboxylic acid salt / Hydrocarbon derivative
Molecular Framework
Aliphatic acyclic compounds
External Descriptors
Not Available
Affected organisms
Not Available

Chemical Identifiers

UNII
5K3UP561AX
CAS number
135998-32-2
InChI Key
BLALCKLYSDDAOC-JWFOFJTQSA-K
InChI
InChI=1S/C14H23N3O10.In/c18-10(19)5-15(1-3-16(6-11(20)21)7-12(22)23)2-4-17(8-13(24)25)9-14(26)27;/h1-9H2,(H,18,19)(H,20,21)(H,22,23)(H,24,25)(H,26,27);/q;+3/p-3/i;1-4
IUPAC Name
(111In)indium(3+) ion 2-[bis({2-[bis(carboxymethyl)amino]ethyl})amino]acetate
SMILES
[111In+3].OC(=O)CN(CCN(CCN(CC([O-])=O)CC([O-])=O)CC([O-])=O)CC(O)=O

References

General References
Not Available
KEGG Drug
D04527
PubChem Compound
131704319
PubChem Substance
347827852
ChemSpider
25048228
Drugs.com
Drugs.com Drug Page
FDA label
Download (2.04 MB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1TerminatedTreatmentNeoplasms, Brain / Tumors of the Central Nervous System1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
SolutionIntrathecal3.75 mCi/1.5mL
SolutionIntrathecal1 mCi/1mL
Prices
Not Available
Patents
Not Available

Properties

State
Not Available
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility5.71 mg/mLALOGPS
logP0.11ALOGPS
logP-6.3ChemAxon
logS-2ALOGPS
pKa (Strongest Acidic)1.95ChemAxon
pKa (Strongest Basic)8.82ChemAxon
Physiological Charge-3ChemAxon
Hydrogen Acceptor Count13ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area204.71 Å2ChemAxon
Rotatable Bond Count16ChemAxon
Refractivity118.96 m3·mol-1ChemAxon
Polarizability34.91 Å3ChemAxon
Number of Rings0ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available

Drug created on November 30, 2015 19:10 / Updated on June 12, 2020 17:42