ioflupane i-123

Small moleculeapprovedImaging agent

Approved

Jan 14, 2011

Ioflupane I-123 (trade name DaTscan) is a radioiodinated cocaine analogue synthesized from a key starting material Sn FP-CT via oxidative iododestannylation with sodium (123I)-iodide. Ioflupane I-123 binds reversibly with high affinity to the dopamine transporter (DaT) protein, a marker for presynaptic terminals in dopaminergic nigrostriatal neurons. It has been developed as a dopamine transporter imaging agent for single photon emission computed tomography (SPECT) which is claimed to be sensitive enough to differentiate changes in the nigrostriatal dopaminergic system in patients with Parkinsonism and healthy controls. DaTSCAN is unable to discriminate between Parkinson's Disease, Multiple System Atrophy and Progressive Supranuclear Palsy. DaTscan is an adjunct to other diagnostic evaluations. Headache, nausea, vertigo, dry mouth, or dizziness of mild to moderate severity as well as hypersensitivity reactions and injection-site pain have been reported. The DaTscan injection may contain up to 6% of free iodide (iodine 123 or I-123). To decrease thyroid accumulation of I-123, the thyroid gland has to be blocked at least one hour before administration of DaTscan because of the long-term risk for thyroid neoplasia. DaTscan was first approved in the European Union (EU) on July 27, 2000. It is also approved in Israel, Switzerland and in the United States (a total of 33 countries). — NCATS

Clinical trial activity

11 trials · 18 clinical orgs · 2 marketing orgs

Phase 1
2
Phase 2
7
Phase 3
4
Phase 4
1

Earliest trial started Nov 1, 2003 (NCT00209456)

Timeline

2000s

  1. Jan 1, 2003

    General Electric — Earliest Phase 3 Sponsor(trial)

  2. Jan 1, 2009

    Earliest Phase 2 Sponsor(trial)

2010s

  1. Jan 14, 2011

    Earliest FDA Approval

  2. Jan 14, 2011

    General Electric — NDA Secondary Org

  3. Jan 24, 2011

    General Electric — First NDA Organization

  4. Jan 24, 2011

    General Electric — NDA Organization

  5. Jan 1, 2012

    Earliest Phase 1 Sponsor(trial)

2020s

  1. Mar 30, 2022

    Curium Pharma — Marketing Organization

Indications

Mechanism of action

Approval history

  • approvedPriority reviewJan 14, 2011

Chemistry & pharmacology

Loading structure…

SMILES

COC(=O)[C@H]1[C@@H](c2ccc(I)cc2)C[C@@H]2CC[C@H]1N2CCCF
Mol. weight
431.29 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Delivery
Parenteral
Availability
Prescription Only
Imaging
123-iodine

Oral

No

Parenteral

Yes

Topical

No

Sources

Also known as

  • 123i fp-cit
  • 123i fp-cit
  • 123i-fp-cit
  • 123i-fp-cit
  • 123i-fp-cit
  • 123i-ioflupane
  • 123i-ioflupane
  • 123i-ioflupane
  • 12 i-fp-cit
  • (18f)fp-cit
  • 2-carbomethoxy-8-(3-fluoropropyl)-3-(4-iodophenyl)tropane
  • beta-cit-fp
  • datscan
  • datscan
  • datscan
  • datscan
  • datscan
  • fluoropropylcarbomethoxyiodophenylnortropane
  • fpcit
  • fp-cit
  • i-123 ioflupane
  • i(123)-n-fluoropropyl-2-beta-carbomethoxy-3-(4-iodophenyl)nortropane
  • i(123)-n-omega-fluoropropyl-2-beta-carbomethoxy-3-beta(4-iodophenyl)nortropane
  • iodine ioflupane (123i)
  • iodine ioflupane (123i)
  • iodine ioflupane (123i)
  • ioflupane
  • ioflupane
  • ioflupane
  • ioflupane
  • ioflupane ((123)i)
  • ioflupane ((123)i)
  • ioflupane (123i)
  • ioflupane (123i)
  • ioflupane (123i)
  • ioflupane (123i)
  • ioflupane (123l)
  • ioflupane i123
  • ioflupane i 123
  • ioflupane i 123
  • ioflupane i 123
  • ioflupane i 123
  • ioflupane i-123
  • ioflupane i-123
  • ioflupane i-123
  • ioflupane i-123
  • ioflupane i-123
  • ioflupane i-123
  • ioflupane i(123)
  • ioflupane i(123)
  • ioflupano (123i)
  • ioflupano (123i)
  • ioflupanum (123i)
  • ioflupanum (123i)
  • l-123 ioflupane
  • n-omega-fluoropropyl-2beta-carbomethoxy-3beta-(4-iodophenyl)tropane
  • (o-methyl-11c)beta-cit-fp
  • v09ab03
  • v09ab03

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT04564092Phase 1Oct 31, 2020General Electric, Jiao Tong University, PPD
NCT04193527Phase 3Dec 31, 2019General Electric, PPD
NCT03185182Phase 2Jun 1, 2017Lund University, Region Skane
NCT01950468Phase 3Apr 1, 2017Navidea Biopharmaceuticals
NCT01160263Phase 3Oct 1, 2012University of Paris
NCT01788696Phase 1Jun 1, 2012Duke University, General Electric
NCT01453127Phase 4Oct 1, 2011Mayo Clinic
NCT01141023Phase 2Jun 1, 2010Coriell Institute for Medical Research, Institute for Neurodegenerative Disorders, Michael J. Fox Foundation for Parkinson's Research, National Institutes of Health (NIH), University of California, Los Angeles, University of Iowa, University of Pennsylvania
NCT00940914Phase 2Mar 1, 2009University of Toulouse
NCT00129181N/AJan 1, 2005General Electric, Institute for Neurodegenerative Disorders, Pfizer
NCT00209456Phase 3Nov 1, 2003General Electric
Showing 11 of 11 trials
Page 1 / 1

Organizations

Research & Development (18)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
General ElectricFor profit5332003
Institute for Neurodegenerative DisordersAcademic/Hospital2122005
PPDFor profit2022019
Coriell Institute for Medical ResearchAcademic/Hospital1012010
Duke UniversityAcademic/Hospital1112012
Jiao Tong UniversityAcademic/Hospital1012020
Lund UniversityAcademic/Hospital1012017
Mayo ClinicAcademic/Hospital1112011
Michael J. Fox Foundation for Parkinson's ResearchAcademic/Hospital1112010
National Institutes of Health (NIH)Government1012010
Navidea BiopharmaceuticalsFor profit1112017
PfizerFor profit1012005
Region SkaneGovernment1112017
University of California, Los AngelesAcademic/Hospital1012010
University of IowaAcademic/Hospital1012010
University of ParisAcademic/Hospital1112012
University of PennsylvaniaAcademic/Hospital1012010
University of ToulouseAcademic/Hospital1112009
18 organizations
Page 1 / 1

Marketing (3)

OrganizationOrg typeRelationshipDate
Curium PharmaFor profitMKTGMar 30, 2022
General ElectricFor profitNDA2Jan 14, 2011
General ElectricFor profitNDAJan 24, 2011