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

Stem definition	Drug id	CAS RN
iodine-containing contrast media	4577	77679-27-7

Description:

Molecule	Description
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

Molecule

Description

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:

Date	Agency	Company	Orphan
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:

Source	Code	Description
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 | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
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 level	Dissociation constant	Type (acidic/basic)
pKa1	10.06	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN	SUBSTRATE				DRUG LABEL	DRUG LABEL

External reference:

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

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Azedra	HUMAN PRESCRIPTION DRUG LABEL	1	71258-015	INJECTION, SOLUTION	15 mCi	INTRAVENOUS	NDA	26 sections
Azedra	HUMAN PRESCRIPTION DRUG LABEL	1	71258-015	INJECTION, SOLUTION	15 mCi	INTRAVENOUS	NDA	26 sections
Azedra	HUMAN PRESCRIPTION DRUG LABEL	1	71258-015	INJECTION, SOLUTION	15 mCi	INTRAVENOUS	NDA	26 sections