ioflupane i-123
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
Earliest trial started Nov 1, 2003 (NCT00209456)
Timeline
2000s
- Jan 1, 2003
General Electric — Earliest Phase 3 Sponsor(trial)
- Jan 1, 2009
Earliest Phase 2 Sponsor(trial)
2010s
- Jan 14, 2011
Earliest FDA Approval
- Jan 14, 2011
General Electric — NDA Secondary Org
- Jan 24, 2011
General Electric — First NDA Organization
- Jan 24, 2011
General Electric — NDA Organization
- Jan 1, 2012
Earliest Phase 1 Sponsor(trial)
2020s
- Mar 30, 2022
Curium Pharma — Marketing Organization
Indications
Approved for
Studied for
- Alzheimer Disease · Phase 3
- Amyotrophic Lateral Sclerosis · Phase 3
- Atrophy · Phase 3
- Carcinoma, Renal Cell · Phase 2
- Cognitive Dysfunction · Phase 4
- Dementia · Phase 4
- Dementia, Vascular · Phase 3
- Essential Tremor · Phase 3
- Healthy Volunteers · Phase 1
- Lewy Body Disease · Phase 3
- Movement Disorders · Phase 4
- Pain · Phase 2
- Parkinson Disease · Phase 3
- Parkinsonian Disorders · Phase 4
- REM Sleep Behavior Disorder · Phase 4
- Supranuclear Palsy, Progressive · Phase 3
Mechanism of action
- Dopamine transporterBINDING AGENT
SLC6A3 binding agent
Approval history
- approvedPriority reviewJan 14, 2011
Chemistry & pharmacology
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
- ChEMBLCHEMBL1945778 ↗
- NCATS3MM99T8R5Q ↗
- ChEMBLCHEMBL2110569 ↗
- ChEMBLCHEMBL2096623 ↗
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 ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT04564092 | Phase 1 | Oct 31, 2020 | General Electric, Jiao Tong University, PPD |
| NCT04193527 | Phase 3 | Dec 31, 2019 | General Electric, PPD |
| NCT03185182 | Phase 2 | Jun 1, 2017 | Lund University, Region Skane |
| NCT01950468 | Phase 3 | Apr 1, 2017 | Navidea Biopharmaceuticals |
| NCT01160263 | Phase 3 | Oct 1, 2012 | University of Paris |
| NCT01788696 | Phase 1 | Jun 1, 2012 | Duke University, General Electric |
| NCT01453127 | Phase 4 | Oct 1, 2011 | Mayo Clinic |
| NCT01141023 | Phase 2 | Jun 1, 2010 | Coriell 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 |
| NCT00940914 | Phase 2 | Mar 1, 2009 | University of Toulouse |
| NCT00129181 | N/A | Jan 1, 2005 | General Electric, Institute for Neurodegenerative Disorders, Pfizer |
| NCT00209456 | Phase 3 | Nov 1, 2003 | General Electric |
Organizations
Research & Development (18)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| General Electric | For profit | 5 | 3 | 3 | 2003 |
| Institute for Neurodegenerative Disorders | Academic/Hospital | 2 | 1 | 2 | 2005 |
| PPD | For profit | 2 | 0 | 2 | 2019 |
| Coriell Institute for Medical Research | Academic/Hospital | 1 | 0 | 1 | 2010 |
| Duke University | Academic/Hospital | 1 | 1 | 1 | 2012 |
| Jiao Tong University | Academic/Hospital | 1 | 0 | 1 | 2020 |
| Lund University | Academic/Hospital | 1 | 0 | 1 | 2017 |
| Mayo Clinic | Academic/Hospital | 1 | 1 | 1 | 2011 |
| Michael J. Fox Foundation for Parkinson's Research | Academic/Hospital | 1 | 1 | 1 | 2010 |
| National Institutes of Health (NIH) | Government | 1 | 0 | 1 | 2010 |
| Navidea Biopharmaceuticals | For profit | 1 | 1 | 1 | 2017 |
| Pfizer | For profit | 1 | 0 | 1 | 2005 |
| Region Skane | Government | 1 | 1 | 1 | 2017 |
| University of California, Los Angeles | Academic/Hospital | 1 | 0 | 1 | 2010 |
| University of Iowa | Academic/Hospital | 1 | 0 | 1 | 2010 |
| University of Paris | Academic/Hospital | 1 | 1 | 1 | 2012 |
| University of Pennsylvania | Academic/Hospital | 1 | 0 | 1 | 2010 |
| University of Toulouse | Academic/Hospital | 1 | 1 | 1 | 2009 |
Marketing (3)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Curium Pharma | For profit | MKTG | Mar 30, 2022 |
| General Electric | For profit | NDA2 | Jan 14, 2011 |
| General Electric | For profit | NDA | Jan 24, 2011 |