Indium In-111 oxyquinoline

Identification

Summary

Indium In-111 oxyquinoline is a radiopharmaceutical diagnostic agent used for radiolabeling autologous leukocytes as an adjunct in the detection of inflammatory processes to which leukocytes migrate.

Brand Names
Indium In 111 Oxyquinoline
Generic Name
Indium In-111 oxyquinoline
DrugBank Accession Number
DB09473
Background

Indium In 111 oxyquinoline (oxine) is a diagnostic radiopharmaceutical intended for radiolabeling of autologous leukocytes. It is composed of a 3:1 saturated complex of In-111 isotope and oxyquinoline. Indium-111 decays by isomeric transition and electron capture to cadmium-111, emitting a gamma ray that can be detected with a gamma ray camera. It is therefore useful in nuclear medicine, and is used in the labeling of leukocytes for localization of processes to which leukocytes migrate, such as those associated with abscesses or other infections. The degree of accuracy may vary with labeling techniques and with the size, location and nature of the inflammatory process.

Following intravenous administration, the lipid-soluble complex is able to penetrate platelet cell membranes. Once inside, Indium detaches from the oxyquinoline complexes and becomes attached to cytoplasmic components.

Type
Small Molecule
Groups
Approved
Structure
Weight
Average: 543.364
Monoisotopic: 543.039927129
Chemical Formula
C27H18InN3O3
Synonyms
  • In-111 oxyquinoline
  • Indium (111 In) oxyquinoline
  • Indium (In111) oxine
  • Indium (In111) oxyquinoline
  • Indium 111In oxyquinoline
  • Indium In-111 oxine
  • Indium In111 oxine
  • Indium-111 oxine
  • Indium-111 oxyquinoline

Pharmacology

Indication

Indium In 111 oxyquinoline is indicated for radiolabeling autologous leukocytes.

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Diagnostic agentInflammatory processes to which leukocytes migrate••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Not Available

Mechanism of action

Indium-111 decays by isomeric transition and electron capture to cadmium-111, emitting a gamma ray that can be detected with a gamma ray camera. Following intravenous administration, the lipid-soluble complex is able to penetrate platelet cell membranes. Once inside, Indium detaches from the oxyquinoline complexes and becomes attached to cytoplasmic components.

Absorption

After injection of labeled leukocytes into normal volunteers, about 30% of the dose is taken up by spleen and 30% by liver, reaching a plateau at 2-48 hours after injection.

Volume of distribution

Not Available

Protein binding

The presence of red blood cells or plasma will lead to reduced leukocyte labeling efficiency as transferrin in plasma competes for indium In 111 oxyquinoline.

Metabolism
Not Available
Route of elimination

Elimination from the body of injected indium In 111 oxyquinoline is probably mainly through decay to stable cadmium since only a negligible amount (less than 1%) of the dose is excreted in feces and urine in 24 hours.

Half-life

Indium In 111 decays by electron capture with a physical half-life of 67.2 hours (2.8 days). Between 9.5 to 24.4% of the injected dose remains in whole blood and clears with a biological half-time of 2.8 to 5.5 hours. The remainder (13-18%) clears from blood with a biological half-time of 64 to 116 hours.

Clearance

Clearance from whole blood and biological distribution can vary considerably with the individual recipient, the condition of the injected cells and labeling techniques used. Clearance from liver and spleen, for the purpose of calculating the radiation dose, is assumed to be equal to the physical half-life of indium In 111 (67.2 hours).

Adverse Effects
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Toxicity

Due to radiation exposure, indium In 111 oxyquinoline labeled leukocytes could cause fetal harm when administered to pregnant women. If this radiopharmaceutical is used during pregnancy, the patient should be informed of the potential hazard to the fetus. Indium In 111 oxyquinoline, like other radioactive drugs, must be handled with care and appropriate safety measures should be used to minimize radiation exposure to clinical personnel. Care should also be taken to minimize radiation exposure to the patient consistent with proper patient management.

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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Active Moieties
NameKindUNIICASInChI Key
Indium cation In-111ionicWJZ06C0H8L131391-70-3RJMMFJHMVBOLGY-AHCXROLUSA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Indium 111 OxyquinoloneSolution2 mCi/1mLIntravenousAnazao Health Corporation2012-06-19Not applicableUS flag
Indium in 111 OxyquinolineSolution1 ug/1mLIntravenousMedi-Physics Inc. dba GE Healthcare.1985-12-01Not applicableUS flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Indium In 111 OxyquinolineLiquid1 mCi/1mLIntravenousBWXT Medical Ltd.2019-09-27Not applicableUS flag
Indium In 111 OxyquinolineLiquid1 mCi/1mLIntravenousNordion (Canada) Inc.2018-12-192018-12-19US flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Indium 111 OxyquinoloneIndium In-111 oxyquinoline (2 mCi/1mL)SolutionIntravenousAnazao Health Corporation2012-06-19Not applicableUS flag

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
LGX9OL562T
CAS number
65389-08-4
InChI Key
AEGSYIKLTCZUEZ-FZTWWWDYSA-K
InChI
InChI=1S/3C9H7NO.In/c3*11-8-5-1-3-7-4-2-6-10-9(7)8;/h3*1-6,11H;/q;;;+3/p-3/i;;;1-4
IUPAC Name
(111In)indium(3+) ion tris(quinolin-8-olate)
SMILES
[111In+3].[O-]C1=CC=CC2=C1N=CC=C2.[O-]C1=CC=CC2=C1N=CC=C2.[O-]C1=CC=CC2=C1N=CC=C2

References

General References
  1. Thakur ML, Welch MJ, Joist JH, Coleman RE: Indium-LLL labeled platelets: studies on preparation and evaluation of in vitro and in vivo functions. Thromb Res. 1976 Oct;9(4):345-57. [Article]
KEGG Drug
D04526
PubChem Compound
119117
PubChem Substance
347827858
ChemSpider
106429
RxNav
1314372
Drugs.com
Drugs.com Drug Page
Wikipedia
Indium-111
FDA label
Download (2.75 MB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
SolutionIntravenous2 mCi/1mL
LiquidIntravenous1 mCi/1mL
SolutionIntravenous1 ug/1mL
Prices
Not Available
Patents
Not Available

Properties

State
Not Available
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00128 mg/mLALOGPS
logP5.38ALOGPS
logP1.83Chemaxon
logS-5.6ALOGPS
pKa (Strongest Acidic)9.36Chemaxon
pKa (Strongest Basic)4.83Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count2Chemaxon
Hydrogen Donor Count0Chemaxon
Polar Surface Area35.95 Å2Chemaxon
Rotatable Bond Count0Chemaxon
Refractivity52.51 m3·mol-1Chemaxon
Polarizability14.48 Å3Chemaxon
Number of Rings6Chemaxon
Bioavailability0Chemaxon
Rule of FiveNoChemaxon
Ghose FilterNoChemaxon
Veber's RuleYesChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available
Chromatographic Properties
Collision Cross Sections (CCS)
Not Available

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