iobenguane (131I) 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
iodine-containing contrast media 4577 77679-27-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • iobenguane (131I)
  • Iobenguane I 131
  • 3-iodobenzylguanidine (131I)
  • raiatt MIBG-I 131
  • azedra
  • 131I-MIBG
AZEDRA is an I 131 labeled iobenguane. Iobenguane is similar in structure to the neurotransmitter norepinephrine (NE) and is subject to the same uptake and accumulation pathways as NE. Iobenguane is taken up by the NE transporter in adrenergic nerve terminals and accumulates in adrenergically innervated tissues, such as the heart, lungs, adrenal medulla, salivary glands, liver, and spleen as well as tumors of neural crest origin. Pheochromocytoma and paraganglioma (PPGL) are tumors of neural crest origin that express high levels of the NE transporter on their cell surfaces. Following intravenous administration, AZEDRA is taken up and accumulates within pheochromocytoma and paraganglioma cells, and radiation resulting from radioactive decay of I 131 causes cell death and tumor necrosis.
  • Molecular weight: 279.10
  • Formula: C8H10IN3
  • CLOGP: 1.55
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 3
  • TPSA: 61.90
  • ALOGS: -3.44
  • ROTB: 2

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
March 25, 1994 FDA PHARMALUCENCE
Sept. 27, 2021 PMDA FUJIFILM TOYAMA CHEMICAL CO., LTD.

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC V09IX02 VARIOUS
DIAGNOSTIC RADIOPHARMACEUTICALS
TUMOUR DETECTION
Other diagnostic radiopharmaceuticals for tumour detection
ATC V10XA02 VARIOUS
THERAPEUTIC RADIOPHARMACEUTICALS
OTHER THERAPEUTIC RADIOPHARMACEUTICALS
Iodine (131I) compounds
FDA MoA N0000000205 Radiopharmaceutical Activity
FDA EPC N0000177914 Radioactive Diagnostic Agent
MeSH PA D000970 Antineoplastic Agents
MeSH PA D064907 Diagnostic Uses of Chemicals
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D007202 Indicators and Reagents
MeSH PA D019275 Radiopharmaceuticals

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Paraganglioma indication 302833002 DOID:0050773
Pheochromocytoma indication 302835009




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.06 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
15mCi/ML AZEDRA PROGENICS PHARMS INC N209607 July 30, 2018 RX SOLUTION INTRAVENOUS July 30, 2025 TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER WITH IOBENGUANE SCAN POSITIVE, UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC PHEOCHROMOCYTOMA OR PARAGANGLIOMA WHO REQUIRE SYSTEMIC ANTICANCER THERAPY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Sodium-dependent noradrenaline transporter Transporter SUBSTRATE DRUG LABEL DRUG LABEL

External reference:

IDSource
4037823 VANDF
CHEBI:135997 CHEBI
CHEMBL1615779 ChEMBL_ID
71184 PUBCHEM_CID
2053281 RXNORM
23656 MMSL
290523 MMSL
d08912 MMSL
001569 NDDF
395789007 SNOMEDCT_US
429328002 SNOMEDCT_US
D03308 KEGG_DRUG
D019797 MESH_DESCRIPTOR_UI
C0524959 UMLSCUI
6088 INN_ID
Q461L7AK4R UNII

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Azedra HUMAN PRESCRIPTION DRUG LABEL 1 71258-015 INJECTION, SOLUTION 15 mCi INTRAVENOUS NDA 26 sections