Identification
- Generic Name
- Iobenguane sulfate I-123
- DrugBank Accession Number
- DB09546
- Background
Iobenguane sulfate I-123 is a radiopharmaceutical used in gamma-scintigraphy of adrenergically inervated tissues [FDA Label].
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Iobenguane sulfate I-123 (DB09546)
- Weight
- Average: 640.26
Monoisotopic: 639.953520274 - Chemical Formula
- C16H22I2N6O4S
- Synonyms
- Iobenguane sulfate I 123
Pharmacology
- Indication
For use in the diagnostic imaging of adrenergically inervated tissues for the purposes of detecting metastatic pheochromocytoma or neuroblastoma [FDA Label]. Also used to assess the sympathetic inervation of the myocardium via determination of the heart to mediastinum ratio of radioactivity in patients with New York Heart Association class II or III heart failure.
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- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- Pharmacodynamics
Iobenguane I-123 is taken up by and stored in adrenergic nerve terminals allowing for the radiographic imaging of adrenergically inervated organs and tissues [FDA Label].
- Mechanism of action
Iobenguane I-123 is transported into adrenergic nerve terminals via the noradrenaline uptake transporter [FDA Label]. It is rapidly cleared from systemic circulation and collected in adrenergically invervated tissues. This allows for gamma-scintigraphic imaging of these tissues and their associated organs for diagnostic purposes.
- Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
Metabolized to m-iodohippuric acid and free radioiodide [FDA Label]. The metabolism of iobenguane I-123 and the enzymes involved has not been well studied.
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- Route of elimination
Primarily eliminated via the urine as the parent compound (70-90%) [FDA Label]. A small amount is eliminated in the urine as m-iodohippuric acid (</10%) and free radioiodide (</6%). Less than 1% is eliminated in the feces. Iobenguane I-123 is initially rapidly cleared from circulation follwed by a slow clearance from other tissues over 4 days. Retention is the longest in highly adrenergically inervated tissues like the adrenal medulla, heart, and salivary glands. Iobenguane I-123 is not cleared by dialysis.
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
As a radiopharmaceutical, iobenguane I-123 carries the risk of radiation toxicity if administered in innappropriately large doses or in patients with renal insufficency [FDA Label]. Fequent voiding of the bladder is encouraged to minimize the radiation dose to the bladder.
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Abacavir may decrease the excretion rate of Iobenguane sulfate I-123 which could result in a higher serum level. Aceclofenac Aceclofenac may decrease the excretion rate of Iobenguane sulfate I-123 which could result in a higher serum level. Acemetacin Acemetacin may decrease the excretion rate of Iobenguane sulfate I-123 which could result in a higher serum level. Acetaminophen Acetaminophen may decrease the excretion rate of Iobenguane sulfate I-123 which could result in a higher serum level. Acetazolamide Acetazolamide may increase the excretion rate of Iobenguane sulfate I-123 which could result in a lower serum level and potentially a reduction in efficacy. Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Iobenguane sulfate I-123 which could result in a higher serum level. Aclidinium Aclidinium may decrease the excretion rate of Iobenguane sulfate I-123 which could result in a higher serum level. Acrivastine Acrivastine may decrease the excretion rate of Iobenguane sulfate I-123 which could result in a higher serum level. Acyclovir Acyclovir may decrease the excretion rate of Iobenguane sulfate I-123 which could result in a higher serum level. Adefovir dipivoxil Adefovir dipivoxil may decrease the excretion rate of Iobenguane sulfate I-123 which could result in a higher serum level. 
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- 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.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image i 123 MIBG meta iodobenzylguanidine Injection, powder, lyophilized, for solution 25 mCi/1 Intravenous Anazao Health Corporation 2012-05-23 Not applicable US 
- Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image i 123 MIBG meta iodobenzylguanidine Iobenguane sulfate I-123 (25 mCi/1) Injection, powder, lyophilized, for solution Intravenous Anazao Health Corporation 2012-05-23 Not applicable US
Categories
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as iodobenzenes. These are aromatic compounds containing one or more iodine atoms attached to a benzene.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Benzene and substituted derivatives
- Sub Class
- Halobenzenes
- Direct Parent
- Iodobenzenes
- Alternative Parents
- Organic sulfuric acids / Aryl iodides / Guanidines / Propargyl-type 1,3-dipolar organic compounds / Carboximidamides / Organopnictogen compounds / Organoiodides / Organic oxides / Hydrocarbon derivatives
- Substituents
- Aromatic homomonocyclic compound / Aryl halide / Aryl iodide / Carboximidamide / Guanidine / Hydrocarbon derivative / Iodobenzene / Organic 1,3-dipolar compound / Organic nitrogen compound / Organic oxide
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 23X1185WBO
- CAS number
- 80663-95-2
- InChI Key
- XNACDNPGABUBFR-FKNPGSCZSA-N
- InChI
- InChI=1S/2C8H10IN3.H2O4S/c2*9-7-3-1-2-6(4-7)5-12-8(10)11;1-5(2,3)4/h2*1-4H,5H2,(H4,10,11,12);(H2,1,2,3,4)/i2*9-4;
- IUPAC Name
- bis(N-{[3-(¹²³I)iodophenyl]methyl}guanidine); sulfuric acid
- SMILES
- OS(O)(=O)=O.NC(=N)NCC1=CC([123I])=CC=C1.NC(=N)NCC1=CC([123I])=CC=C1
References
- General References
- Not Available
- External Links
- PubChem Compound
- 56840904
- PubChem Substance
- 347827877
- ChemSpider
- 32701571
- 1427223
- ChEMBL
- CHEMBL3989523
- FDA label
- Download (302 KB)
- MSDS
- Download (100 KB)
Clinical Trials
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, powder, lyophilized, for solution Intravenous 25 mCi/1 - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Liquid
- Experimental Properties
Property Value Source water solubility Soluble MSDS Radioactivity (mCi/mL) 2 MSDS - Predicted Properties
Property Value Source Water Solubility 0.1 mg/mL ALOGPS logP 1.42 ALOGPS logP 1.69 ChemAxon logS -3.4 ALOGPS pKa (Strongest Basic) 11.75 ChemAxon Physiological Charge 1 ChemAxon Hydrogen Acceptor Count 3 ChemAxon Hydrogen Donor Count 3 ChemAxon Polar Surface Area 61.9 Å2 ChemAxon Rotatable Bond Count 4 ChemAxon Refractivity 68.61 m3·mol-1 ChemAxon Polarizability 21.91 Å3 ChemAxon Number of Rings 2 ChemAxon Bioavailability 1 ChemAxon Rule of Five No ChemAxon Ghose Filter No ChemAxon Veber's Rule No ChemAxon MDDR-like Rule No ChemAxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Norepinephrine:sodium symporter activity
- Specific Function
- Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals.
- Gene Name
- SLC6A2
- Uniprot ID
- P23975
- Uniprot Name
- Sodium-dependent noradrenaline transporter
- Molecular Weight
- 69331.42 Da
Drug created at November 30, 2015 19:10 / Updated at October 06, 2020 17:43