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.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Diagnostic agent Inflammatory processes to which leukocytes migrate •••••••••••• - Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- 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
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- 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
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Active Moieties
Name Kind UNII CAS InChI Key Indium cation In-111 ionic WJZ06C0H8L 131391-70-3 RJMMFJHMVBOLGY-AHCXROLUSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Indium 111 Oxyquinolone Solution 2 mCi/1mL Intravenous Anazao Health Corporation 2012-06-19 Not applicable US Indium in 111 Oxyquinoline Solution 1 ug/1mL Intravenous Medi-Physics Inc. dba GE Healthcare. 1985-12-01 Not applicable US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Indium In 111 Oxyquinoline Liquid 1 mCi/1mL Intravenous BWXT Medical Ltd. 2019-09-27 Not applicable US Indium In 111 Oxyquinoline Liquid 1 mCi/1mL Intravenous Nordion (Canada) Inc. 2018-12-19 2018-12-19 US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Indium 111 Oxyquinolone Indium In-111 oxyquinoline (2 mCi/1mL) Solution Intravenous Anazao Health Corporation 2012-06-19 Not applicable US
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
- 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]
- External Links
- KEGG Drug
- D04526
- PubChem Compound
- 119117
- PubChem Substance
- 347827858
- ChemSpider
- 106429
- 1314372
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Indium-111
- FDA label
- Download (2.75 MB)
Clinical Trials
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Solution Intravenous 2 mCi/1mL Liquid Intravenous 1 mCi/1mL Solution Intravenous 1 ug/1mL - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Not Available
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.00128 mg/mL ALOGPS logP 5.38 ALOGPS logP 1.83 Chemaxon logS -5.6 ALOGPS pKa (Strongest Acidic) 9.36 Chemaxon pKa (Strongest Basic) 4.83 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 35.95 Å2 Chemaxon Rotatable Bond Count 0 Chemaxon Refractivity 52.51 m3·mol-1 Chemaxon Polarizability 14.48 Å3 Chemaxon Number of Rings 6 Chemaxon Bioavailability 0 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - 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