Ioflupane I-123
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Identification
- Summary
Ioflupane I-123 is a radiopharmaceutical used in single photon emission computed tomography (SPECT) brain imaging to help diagnose patients with suspected Parkinsonian syndromes.
- Brand Names
- Datscan
- Generic Name
- Ioflupane I-123
- DrugBank Accession Number
- DB08824
- Background
Ioflupane (I-123) is a radiopharmaceutical used to image dopamine neurons and diagnose Parkinsonian syndromes.
- Type
- Small Molecule
- Groups
- Approved
- Structure
- Weight
- Average: 427.291
Monoisotopic: 427.076880092 - Chemical Formula
- C18H23FINO2
- Synonyms
- 123I-FP-CIT
- 123I-Ioflupane
- Iodine ioflupane (123I)
- Ioflupane ((123)I)
- Ioflupane (123I)
- Ioflupane I 123
- Ioflupane I(123)
- Ioflupano (123I)
- Ioflupanum (123I)
Pharmacology
- Indication
Ioflupane I-123 is a SPECT (single photon emission computerized tomography) agent used to distinguish between Parkinson’s syndrome tremors and essential tremor.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Diagnostic agent Parkinsonian syndromes •••••••••••• - Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
iodine-123 labeled ioflupanebinds selectively to striatal presynaptic dopamine neurons by binding reversibly to presynaptic dopamine transporters.
- Mechanism of action
Iodine-123 labeled ioflupane binds to presynaptic dopamine transporters. When Iodine-123 decays, a gammay ray is emmitted and detected through SPECT.
Target Actions Organism ASodium-dependent dopamine transporter modulatorHumans - Absorption
Absorption is 100% because administered I.V.
- Volume of distribution
Compared to the entire brain, about 30% of radioactivity is taken up by the striatum.
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
About 60% is excreted in the urine and 14% in the feces after 48 hours.
- Half-life
Half life is 13.2 hours.
- Clearance
Not Available
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
Not Available
- 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 Ioflupane I-123 which could result in a higher serum level. Aceclofenac Aceclofenac may decrease the excretion rate of Ioflupane I-123 which could result in a higher serum level. Acemetacin Acemetacin may decrease the excretion rate of Ioflupane I-123 which could result in a higher serum level. Acetaminophen Acetaminophen may decrease the excretion rate of Ioflupane I-123 which could result in a higher serum level. Acetazolamide Acetazolamide may increase the excretion rate of Ioflupane I-123 which could result in a lower serum level and potentially a reduction in efficacy. - Food Interactions
- Take with or without food.
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 Celsunax Injection, solution 74 MBq/ml Intravenous Pinax Pharma Gmbh 2021-10-26 Not applicable EU Celsunax Injection, solution 74 MBq/ml Intravenous Pinax Pharma Gmbh 2021-10-26 Not applicable EU Datscan Injection, solution 74 MBq/ml Intravenous Ge Healthcare S.R.L. 2016-09-08 Not applicable EU DaTscan Injection, solution 2 mCi/1mL Intravenous Medi-Physics, Inc. dba GE Healthcare 2011-03-01 Not applicable US Datscan Injection, solution 74 MBq/ml Intravenous Ge Healthcare S.R.L. 2016-09-08 Not applicable EU - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ioflupane I 123 Injection, solution 2 mCi/1mL Intravenous Curium Netherlands B.V. 2022-03-31 Not applicable US
Categories
- ATC Codes
- V09AB03 — Iodine ioflupane (123i)
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as phenyltropanes. These are compounds containing a phenyl group linked to a tropane moiety. Tropane is an organonitrogenous [3.2.1] bicyclic organic compound.
- Kingdom
- Organic compounds
- Super Class
- Alkaloids and derivatives
- Class
- Tropane alkaloids
- Sub Class
- Phenyltropanes
- Direct Parent
- Phenyltropanes
- Alternative Parents
- Phenylpiperidines / Piperidinecarboxylic acids / Aralkylamines / Iodobenzenes / Aryl iodides / N-alkylpyrrolidines / Methyl esters / Trialkylamines / Amino acids and derivatives / Azacyclic compounds show 8 more
- Substituents
- Alkyl fluoride / Alkyl halide / Amine / Amino acid or derivatives / Aralkylamine / Aromatic heteropolycyclic compound / Aryl halide / Aryl iodide / Azacycle / Benzenoid show 27 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- organofluorine compound, azabicycloalkane, methyl ester (CHEBI:68855)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 3MM99T8R5Q
- CAS number
- 155798-07-5
- InChI Key
- HXWLAJVUJSVENX-HFIFKADTSA-N
- InChI
- InChI=1S/C18H23FINO2/c1-23-18(22)17-15(12-3-5-13(20)6-4-12)11-14-7-8-16(17)21(14)10-2-9-19/h3-6,14-17H,2,7-11H2,1H3/t14-,15+,16+,17-/m0/s1/i20-4
- IUPAC Name
- methyl (1R,2S,3S,5S)-8-(3-fluoropropyl)-3-[4-(¹²³I)iodophenyl]-8-azabicyclo[3.2.1]octane-2-carboxylate
- SMILES
- [H][C@]12CC[C@]([H])([C@H]([C@H](C1)C1=CC=C([123I])C=C1)C(=O)OC)N2CCCF
References
- General References
- Tolosa E, Borght TV, Moreno E: Accuracy of DaTSCAN (123I-Ioflupane) SPECT in diagnosis of patients with clinically uncertain parkinsonism: 2-year follow-up of an open-label study. Mov Disord. 2007 Dec;22(16):2346-51. [Article]
- Benamer TS, Patterson J, Grosset DG, Booij J, de Bruin K, van Royen E, Speelman JD, Horstink MH, Sips HJ, Dierckx RA, Versijpt J, Decoo D, Van Der Linden C, Hadley DM, Doder M, Lees AJ, Costa DC, Gacinovic S, Oertel WH, Pogarell O, Hoeffken H, Joseph K, Tatsch K, Schwarz J, Ries V: Accurate differentiation of parkinsonism and essential tremor using visual assessment of [123I]-FP-CIT SPECT imaging: the [123I]-FP-CIT study group. Mov Disord. 2000 May;15(3):503-10. [Article]
- Link [Link]
- External Links
- KEGG Drug
- D10014
- PubChem Compound
- 3086674
- PubChem Substance
- 175427106
- ChemSpider
- 2343241
- 1426874
- ChEBI
- 68855
- ChEMBL
- CHEMBL3989517
- ZINC
- ZINC000100091991
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Ioflupane_(123I)
- FDA label
- Download (655 KB)
- MSDS
- Download (97.7 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Completed Not Available Parkinson's Disease (PD) 2 somestatus stop reason just information to hide Not Available Unknown Status Not Available Motor Skills Disorders / Parkinson's Disease (PD) 1 somestatus stop reason just information to hide 4 Enrolling by Invitation Diagnostic Dementia / Mild Cognitive Impairment (MCI) / Parkinsonism / Rapid Eye Movement Sleep Behavior Disorder 1 somestatus stop reason just information to hide 3 Completed Diagnostic Alzheimer’s / Dementia With Lewy Body Disease / Non-DLB Dementia / Vascular Dementia (VaD) 1 somestatus stop reason just information to hide 3 Completed Diagnostic Amyotrophic Lateral Sclerosis (ALS) 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, solution Injection, solution Intravenous Injection, solution Intravenous 2 mCi/1mL Injection 74 MBq/mL Injection, solution Intravenous 74 MBq/mL Injection, solution Parenteral 74 MBq/ml Injection, solution 74 MBQ/ML - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5310912 No 1994-05-10 2013-02-25 US
Properties
- State
- Liquid
- Experimental Properties
Property Value Source melting point (°C) 82-83 Not Available water solubility Soluble in water Not Available - Predicted Properties
Property Value Source Water Solubility 0.00566 mg/mL ALOGPS logP 4.24 ALOGPS logP 3.7 Chemaxon logS -4.9 ALOGPS pKa (Strongest Basic) 9.46 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 29.54 Å2 Chemaxon Rotatable Bond Count 6 Chemaxon Refractivity 97.34 m3·mol-1 Chemaxon Polarizability 38.75 Å3 Chemaxon Number of Rings 3 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9761 Blood Brain Barrier + 0.9729 Caco-2 permeable + 0.5307 P-glycoprotein substrate Non-substrate 0.5154 P-glycoprotein inhibitor I Inhibitor 0.7921 P-glycoprotein inhibitor II Inhibitor 0.6468 Renal organic cation transporter Inhibitor 0.7311 CYP450 2C9 substrate Non-substrate 0.7871 CYP450 2D6 substrate Non-substrate 0.6487 CYP450 3A4 substrate Substrate 0.5905 CYP450 1A2 substrate Inhibitor 0.5832 CYP450 2C9 inhibitor Non-inhibitor 0.6451 CYP450 2D6 inhibitor Non-inhibitor 0.5706 CYP450 2C19 inhibitor Non-inhibitor 0.5324 CYP450 3A4 inhibitor Non-inhibitor 0.8127 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.5778 Ames test Non AMES toxic 0.7173 Carcinogenicity Non-carcinogens 0.927 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 2.8764 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.7236 hERG inhibition (predictor II) Inhibitor 0.6662
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-001i-0000900000-38191d83bea9ed2f09ca Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-001i-0000900000-1c41656bb516f289e853 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-001i-0108900000-4955d285e5c0ddd845b0 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-001i-0002900000-f90b2d7debbdb9c81325 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-004i-0900000000-5dc5b1fff481213dd1ac Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0w30-0359800000-eb1ae6ee4215bfa51bde Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 185.5334 predictedDeepCCS 1.0 (2019) [M+H]+ 187.92894 predictedDeepCCS 1.0 (2019) [M+Na]+ 193.84149 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Modulator
- General Function
- Mediates sodium- and chloride-dependent transport of dopamine (PubMed:10375632, PubMed:11093780, PubMed:1406597, PubMed:15505207, PubMed:19478460, PubMed:8302271). Also mediates sodium- and chloride-dependent transport of norepinephrine (also known as noradrenaline) (By similarity). Regulator of light-dependent retinal hyaloid vessel regression, downstream of OPN5 signaling (By similarity)
- Specific Function
- amine binding
- Gene Name
- SLC6A3
- Uniprot ID
- Q01959
- Uniprot Name
- Sodium-dependent dopamine transporter
- Molecular Weight
- 68494.255 Da
References
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- General Function
- Mediates sodium- and chloride-dependent transport of dopamine (PubMed:10375632, PubMed:11093780, PubMed:1406597, PubMed:15505207, PubMed:19478460, PubMed:8302271). Also mediates sodium- and chloride-dependent transport of norepinephrine (also known as noradrenaline) (By similarity). Regulator of light-dependent retinal hyaloid vessel regression, downstream of OPN5 signaling (By similarity)
- Specific Function
- amine binding
- Gene Name
- SLC6A3
- Uniprot ID
- Q01959
- Uniprot Name
- Sodium-dependent dopamine transporter
- Molecular Weight
- 68494.255 Da
References
- Link [Link]
Drug created at December 27, 2012 21:00 / Updated at August 26, 2024 19:24