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Ioflupane I-123 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| iodine-containing contrast media | 4230 | 155798-07-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.180 | High | 0.84 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.673 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 27.990 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 24.774 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 6.280 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 15.460 | % | High | 1 |
| herg | hERG pIC50 | 6.181 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 27.733 | uL/min/10^6 cells | High | 0.84 |
| hlm-clint | Human liver microsomal intrinsic clearance | 107.647 | uL/min/mg protein | High | 0.84 |
| hppb | Human plasma protein binding (% unbound) | 6.180 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT1,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPKAPK2,MET,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ZAP70 | 45 | |||
| kinase-selectivity-class | EIF2AK3,GRK2,MAP2K6 | 3 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.755 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 111.173 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 7.170 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 2.649 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 13.760 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 144.212 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 28.430 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 4.440 | % | High | 0.84 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 148.936 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| 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)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Dopamine transporter scintigraphy abnormal | 77.36 | 67.94 | 6 | 14 | 8 | 42621307 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Dopamine transporter scintigraphy abnormal | 136.49 | 93.70 | 11 | 50 | 22 | 110589216 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| FDA MoA | N0000000205 | Radiopharmaceutical Activity |
| FDA EPC | N0000177914 | Radioactive Diagnostic Agent |
| CHEBI has role | CHEBI:35232 | radiopharmaceuticals |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 7.9 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Sodium-dependent dopamine transporter | Transporter | BINDING AGENT | Ki | 9.21 | DRUG LABEL | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| 4030845 | VUID |
| N0000182831 | NUI |
| 4030845 | VANDF |
| C1956796 | UMLSCUI |
| 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 |
| CHEBI:68855 | CHEBI |
| 3MM99T8R5Q | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| DaTscan | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17156-210 | INJECTION, SOLUTION | 2 mCi | INTRAVENOUS | NDA | 31 sections |
| Ioflupane I 123 | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69945-166 | INJECTION, SOLUTION | 2 mCi | INTRAVENOUS | ANDA | 29 sections |