fluorodopa

Trade name: fluorodopa F18

Small moleculeapprovedImaging agent

Approved

Oct 10, 2019

Fluorodopa F-18 is the amino acid analog fluorodopa (FDOPA) labeled with fluorine F 18, a positron-emitting isotope. It is diagnostic PET agent, which has been used for decades in imaging the loss of dopaminergic neurons in Parkinson's disease, and more recently to detect, stage and restage neuroendocrine tumours and to search for recurrence of viable glioma tissue. Fluorodopa F-18 is able to cross the blood-brain barrier and is taken up by brain tumor cells. As uptake is higher in tumor cells, tumors may then be imaged using positron emission tomography (PET). Assessing tumor uptake of FDOPA may be beneficial for diagnosis, localization and in determining further treatment. The clinical usefulness of Fluorodopa F-18 has been evaluated and recognised in France and subsequently in several EU countries. Fluorodopa F-18 was registered in France in 2006. 6-fluoro-(18F)-L-3,4-dihydroxyphenylalanine (FDOPA) is a large, neutral amino acid that is transported into presynaptic neurons, where it is converted by the enzyme aromatic aminoacid decarboxylase [AAAD]) into fluorodopamine-(18F), which subsequently enters cathecholamine-storage vesicles. 6-fluoro(18F)-L-dopa crosses the blood-brain barrier; therefore, when injected into the blood stream, it reaches the dopaminergic cells in the brain and is used by the brain as a precursor for dopamine. This makes it possible to monitor intracerebral synthesis and uptake of dopamine by means of the positron-emitting 6-fluoro(18F)-L-3,4-dihydroxyphenylalanine (FDOPA), in conjunction with externally-placed devices suited for detection of annihilation photons, which progressively led to the most recent positron emission tomography (PET) units. Iasodopa, the commercial preparation of FDOPA that obtained a marketing authorisation in France in November 2006 (which is currently recognised by several other EU countries), is a solution for injection. The activity available at time of administration ranges from 0.1 GBq to 0.8 GBq per vial. The half-life of the radionuclide is 109.8 min with emission of positron radiation (Emax: 0.633 MeV) followed by photon annihilation radiations of 0.511 MeV. — NCATS

Clinical trial activity

46 trials · 41 clinical orgs · 1 marketing orgs

Phase 1
10
Phase 2
23
Phase 3
4
Phase 4
1

Earliest trial started Dec 15, 1993 (NCT00001277)

Timeline

1990s

  1. Jan 1, 1993

    Earliest Phase 2 Sponsor(trial)

  2. Jan 1, 1999

    Earliest Phase 1 Sponsor(trial)

2010s

  1. Jan 1, 2017

    Earliest Phase 3 Sponsor(trial)

  2. Oct 10, 2019

    Feinstein Institute for Medical Research — Earliest FDA Approval

  3. Oct 10, 2019

    Feinstein Institute for Medical Research — Marketing Organization

  4. Oct 10, 2019

    Feinstein Institute for Medical Research — NDA Organization

Indications

Approved for

Mechanism of action

  • Unspecified targetOTHER

    Diagnostic agent

    Radioactive diagnostic agent for use in position emmission tomography (PET). In dopaminergic nerve terminals in the brain, Fluorodopa (FDOPA) F 18 is decarboxylated to Fluorodopamine (FDA) F 18 which accumulates in the striatum and can be detected in the PET scan.

  • DDC substrate

Approval history

  • approvedOct 10, 2019

Chemistry & pharmacology

Loading structure…

SMILES

N[C@@H](Cc1cc(O)c(O)cc1F)C(=O)O
Mol. weight
215.18 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Availability
Prescription Only
Imaging
18-fluorine

Oral

No

Parenteral

No

Topical

No

Sources

Also known as

  • 18f
  • (18)f-dopa
  • 18 f-dopa
  • 18 f-dopa
  • 18f dopa
  • 18f-dopa
  • 18f-fdopa
  • 18f fluoro-dopa
  • 2-fluoro-5-hydroxytyrosine
  • 3-(2-fluoro-(18)f-4,5-dihydroxyphenyl)-l-alanine
  • 3,4-dihydroxy-6-fluorophenylalanine
  • 6-(18f)fluoro-l-3,4-dihydroxyphenylalanine
  • 6-(18f)fluoro-l-dopa
  • 6-[18]-fluorodopamine
  • 6-[f-18]-fluoro-l-3,4,-dihydroxyphenylalanine
  • 6-fluorodopa
  • 6-fluoro-dopa
  • f-dopa
  • fluorine-18-l-dihydroxyphenylalanine
  • fluorodopa
  • fluorodopa
  • fluorodopa
  • fluorodopa
  • fluorodopa (18f)
  • fluorodopa (18f)
  • fluorodopa (18f)
  • fluorodopa (18f)
  • fluorodopa (18f)
  • fluorodopa f 18
  • fluorodopa f 18
  • fluorodopa f 18
  • fluorodopa f 18
  • fluorodopa f 18, (18)f-labeled cpd

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07025226Early Phase 1 (Phase 1)Aug 12, 2025Mayo Clinic
NCT06667726Phase 2Nov 11, 2024Mayo Clinic
NCT05835258N/AMay 30, 2023Eurecat
NCT05781321Phase 2Mar 23, 2023Mayo Clinic
NCT05512403Phase 3Jan 30, 2023Aix-University of Marseille, François Rabelais University, Institut de Cancerologie Strasbourg Europe, University of Grenoble, University of Lille, University of Lorraine, University of Lyon, University of Nantes, University of Nimes, University of Paris, University of Western Brittany
NCT05906563Phase 2Dec 14, 2022Mansoura University
NCT06053385N/AFeb 9, 2022University of Redlands
NCT05762172N/AFeb 1, 2022University of Picardie Jules Verne
NCT05103618Phase 2Nov 25, 2021Thomas Jefferson University
NCT05759429N/AApr 29, 2021Istituto Auxologico Italiano
NCT04706910Phase 3Jan 20, 2021University of Alberta
NCT05976451N/AOct 1, 2020Ain Shams University
NCT05088798Phase 2Sep 10, 2020Washington University in St. Louis
NCT04459052Phase 2Apr 30, 2020Thomas Jefferson University
NCT05759416Phase 4Apr 1, 2020Al Azhar University
NCT04246437Phase 1Feb 1, 2020Vanderbilt University
NCT03998852Phase 3Jul 1, 2019University of Bordeaux
NCT03778294Phase 2Mar 28, 2019Mayo Clinic, National Cancer Institute (NCI)
NCT03581305Phase 1Nov 20, 2018National Institutes of Health (NIH)
NCT03636945N/AOct 31, 2018Aix-University of Marseille
Showing 20 of 46 trials
Page 1 / 3

Organizations

Research & Development (41)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Mayo ClinicAcademic/Hospital9932010
National Institutes of Health (NIH)Government5521999
National Cancer Institute (NCI)Government4022010
National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)Government3111993
University of PennsylvaniaAcademic/Hospital3322004
Washington University in St. LouisAcademic/Hospital3322013
Aix-University of MarseilleAcademic/Hospital2122018
Methodist Cancer Center, Houston, TexasAcademic/Hospital2122012
Thomas Jefferson UniversityAcademic/Hospital2212020
University of AlbertaAcademic/Hospital2212017
University of California, Los AngelesAcademic/Hospital2122012
Ain Shams UniversityAcademic/Hospital1112020
Al Azhar UniversityAcademic/Hospital1112020
Assistance Publique - Hôpitaux de ParisAcademic/Hospital1112007
Baylor UniversityAcademic/Hospital1112015
Brains Together for the CureAcademic/Hospital1012014
Cook Children's Medical CenterAcademic/Hospital1112013
EurecatFor profit1112023
François Rabelais UniversityAcademic/Hospital1012023
Institut de Cancerologie Strasbourg EuropeAcademic/Hospital1012023
41 organizations
Page 1 / 3

Marketing (2)

OrganizationOrg typeRelationshipDate
Feinstein Institute for Medical ResearchAcademic/HospitalMKTGOct 10, 2019
Feinstein Institute for Medical ResearchAcademic/HospitalNDAOct 10, 2019