Ioflupane I-123 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
iodine-containing contrast media 4230 155798-07-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • Ioflupane I 123
  • DaTSCAN
  • Ioflupane I-123
  • Ioflupane (123I)
Ioflupane binds reversibly to the human recombinant dopamine transporter (DaT). Following administration of DaTscan to humans, radioactive decay of the iodine 123 emits gamma radiation which can be detected externally using gamma detectors, allowing visualization of the brain striata through SPECT imaging. Autoradiography of post-mortem human brain slices exposed to radiolabeled ioflupane shows concentration of the radiolabel in striatum (caudate nucleus and putamen). The specificity of the binding of ioflupane I 125 to dopamine transporter was demonstrated by competition studies with the DaT inhibitor GBR 12909 (a dopamine reuptake inhibitor), the serotonin reuptake inhibitor citalopram, and the norepinephrine reuptake inhibitor desipramine in post-mortem human brain slices exposed to radiolabeled ioflupane. Citalopram reduced binding in the neocortex and thalamus with only minor effects in the striatum. This indicated that the binding in the cortex and thalamus is mainly to the serotonin reuptake sites. Desipramine showed no effect on the level of striatal binding of ioflupane I 125, but reduced extrastriatal binding by 60 to 85%. The binding of ioflupane I 125 to the striatum was abolished in the presence of high concentrations of GBR 12909, indicating selectivity of ioflupane binding for the pre-synaptic DaT.
  • Molecular weight: 427.29
  • Formula: C18H23FINO2
  • CLOGP: 4.42
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 0
  • TPSA: 29.54
  • ALOGS: -4.88
  • ROTB: 6

  • Status: OFP

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

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
June 25, 2019 EMA CIS bio international
Jan. 14, 2011 FDA GE HLTHCARE INC

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
FDA MoA N0000000205 Radiopharmaceutical Activity
FDA EPC N0000177914 Radioactive Diagnostic Agent
CHEBI has role CHEBI:35232 radiopharmaceuticals

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Striatal dopamine transporter visualization using single photon emission computed tomography indication 105371005




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.9 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Sodium-dependent dopamine transporter Transporter BINDING AGENT Ki 9.21 DRUG LABEL DRUG LABEL

External reference:

IDSource
4030845 VUID
N0000182831 NUI
4030845 VANDF
C1956796 UMLSCUI
CHEBI:68855 CHEBI
CHEMBL3989517 ChEMBL_ID
DB08824 DRUGBANK_ID
7500 INN_ID
3MM99T8R5Q UNII
3086674 PUBCHEM_CID
1426874 RXNORM
179428 MMSL
22309 MMSL
d05895 MMSL
013745 NDDF
428122004 SNOMEDCT_US
429296007 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
DaTscan HUMAN PRESCRIPTION DRUG LABEL 1 17156-210 INJECTION, SOLUTION 2 mCi INTRAVENOUS NDA 27 sections
DaTscan HUMAN PRESCRIPTION DRUG LABEL 1 17156-210 INJECTION, SOLUTION 2 mCi INTRAVENOUS NDA 27 sections
Ioflupane I 123 HUMAN PRESCRIPTION DRUG LABEL 1 69945-166 INJECTION, SOLUTION 2 mCi INTRAVENOUS ANDA 25 sections