Fluoride ion F-18

Identification

Name
Fluoride ion F-18
Accession Number
DB09398
Description

Sodium Fluoride F 18 Injection is a positron emitting radiopharmaceutical, no-carrier added. It contains radioactive fluoride F 18 that is used for diagnostic purposes in conjunction with positron emission tomography (PET) imaging and is administered by intravenous injection. Its primary indication is for bone imaging. Increased deposition around joints can occur in arthritis and following trauma and increased deposition in bone has been noted around fracture sites, in osteomyelitis, fibrous dysplasia, spondylitis tuberculosa, and Paget's disease. No adverse reactions have been reported.

Type
Small Molecule
Groups
Approved
Structure
Thumb
Weight
Average: 18.0015
Monoisotopic: 18.001486247
Chemical Formula
F
Synonyms
  • (18F)-Fluoride
  • 18F-Fluoride
  • Fluoride-18 anion

Pharmacology

Indication

18F is used as a bone imaging agent to define areas of altered osteogenic activity. It has been indicated for back pain and otherwise unexplained bone pain, child abuse, abnormal radiographic or laboratory findings, osteomyelitis, trauma, inflammatory and degenerative arthritis, avascular necrosis. Osteonecrosis of the mandible, condylar hyperplasia, and metabolic bone disease are also among the indications for fluoride imaging.

Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

Deposition of 18F fluoride in bone appears to be primarily a function of blood flow to the bone and the efficiency of the bone in extracting the 18F from the blood perfusing the bone. Increased fluorine F 18 ion deposition around joints can occur in arthritis or following trauma; increased deposition has also been documented in bone around fracture sites, in osteomyelities, fibrous dysplasia, spondylitis tuberculosa, Paget's disease, hyperstosis frontalis interna, myositis, ossificans, and in rapidly growing epiphyses. The tendency for fluorine F 18 ions to accumulate in the vicinity of primary and metastatic malignancy in bone has proven clinically useful in detection of such lesions

Mechanism of action

18F-fluoride is a highly sensitive bone-seeking PET tracer used for detection of skeletal abnormalities. The uptake mechanism of 18F-fluoride has better pharmacokinetic characteristics (compared to other elements) including faster blood clearance and 2-fold higher uptake in bone. Uptake of 18F-fluoride reflects blood flow and bone remodeling.

Absorption

Following intravenous administration, Sodium Fluoride F 18 injection provides fluorine F 18 ions that rapidly equilibrate, primarily within the extracellular fluid space.

Volume of distribution

0.5-0.7 L/Kg

Protein binding

Fluorine F 18 ions do not appear to be bound to serum proteins

Metabolism

First, the 18F- exchanges for an OH- ion on the surface of the hydroxyapatite matrix of bone and this is followed by migration of the 18F- into the crystalline matrix of the bone where it is retained until the bone is remodelled.

Route of elimination

Fluorine F 18 ions are rapidly eliminated via the renal system. 20% or more of the fluorine F 18 ions are cleared from the body in the urine within the first 2 hours after intravenous administration.

Half-life

110 min.

Clearance

Renal clearance for fluoride is 48-147 mL/min, depending upon urinary flow and pH.

Adverse Effects
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Toxicity

The lethal dose of NaF to the average adult has been estimated to be between 32 to 64 mg fluoride/kg body weight.

Affected organisms
  • Humans and other mammals
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.
Not Available
Food Interactions
No interactions found.

Products

Product Ingredients
IngredientUNIICASInChI Key
Sodium fluoride F-189L75099X6R22554-99-0PUZPDOWCWNUUKD-ULWFUOSBSA-M
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Sodium Fluoride F 18Injection, solution475 mCi/1mLIntravenousTriad Isotopes, Inc.2010-11-202010-11-20US flag
Sodium FluorideF 18 F 18Injection200 mg/1mLIntravenousChildren's Hospital Of Michigan2012-06-12Not applicableUS flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Sodium Fluoride F 18Injection200 mCi/1mLIntravenousEssential Isotopes LLC2011-01-01Not applicableUS flag
Sodium Fluoride F 18Injection10 mCi/1mLIntravenousGlobal Isotopes, Llc D/B/A Zevacor Molecular2014-10-312019-05-17US flag
Sodium Fluoride F 18Injection, solution200 mCi/1mLIntravenousJUBILANT DRAX IMAGE RADIOPHARMACIES, INC. DBA JUBILANT RADIOPHARMA2011-01-26Not applicableUS flag
Sodium Fluoride F 18Injection, solution200 mCi/1mLIntravenousBiomedial Research Foundation Of Northwest Lousiansa2015-01-22Not applicableUS flag
Sodium Fluoride F 18Injection200 mCi/1mLIntravenousSpectron Mrc, Llc2015-04-24Not applicableUS flag
Sodium Fluoride F 18Injection600 mCi/1mLIntravenousTHE FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH2014-11-19Not applicableUS flag
Sodium Fluoride F 18Injection200 mCi/1mLIntravenousShertech Laboratories, Llc2011-03-23Not applicableUS flag
Sodium Fluoride F 18Injection, solution200 mCi/1mLIntravenousPetnet Solutions, Inc.2011-01-26Not applicableUS flag
Sodium Fluoride F 18Injection200 mCi/1mLIntravenousHouston Cyclotron Partners Lp Dba Cyclotope2011-12-082020-05-11US flag
Sodium Fluoride F 18Injection91.5 mCi/1mLIntravenousMayo Clinic2013-06-28Not applicableUS flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Sodium Fluoride F 18Sodium fluoride F-18 (475 mCi/1mL)Injection, solutionIntravenousTriad Isotopes, Inc.2010-11-202010-11-20US flag
Sodium FluorideF 18 F 18Sodium fluoride F-18 (200 mg/1mL)InjectionIntravenousChildren's Hospital Of Michigan2012-06-12Not applicableUS flag

Categories

ATC Codes
V09IX06 — Sodium fluoride (18f)
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of inorganic compounds known as homogeneous halogens. These are inorganic non-metallic compounds in which the largest atom is a nobel gas.
Kingdom
Inorganic compounds
Super Class
Homogeneous non-metal compounds
Class
Homogeneous halogens
Sub Class
Not Available
Direct Parent
Homogeneous halogens
Alternative Parents
Not Available
Substituents
Homogeneous halogen
Molecular Framework
Not Available
External Descriptors
Not Available

Chemical Identifiers

UNII
4M4WE5N2GE
CAS number
67862-54-8
InChI Key
KRHYYFGTRYWZRS-BJUDXGSMSA-M
InChI
InChI=1S/FH/h1H/p-1/i1-1
IUPAC Name
(18F)fluoride
SMILES
[18F-]

References

General References
  1. article [Link]
  2. drug label [Link]
  3. article [Link]
  4. article [Link]
PubChem Compound
23690531
PubChem Substance
347827843
ChemSpider
8373100
RxNav
1546273
ChEMBL
CHEMBL1248

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Not Yet RecruitingPreventionAtherosclerosis / Cardiovascular Heart Disease / Molecular Imaging1
3Active Not RecruitingDiagnosticBone Metastases From Breast or Prostate Cancer1
2CompletedDiagnosticMalignancies1
2CompletedDiagnosticProstate Neoplasms1
2RecruitingDiagnosticCarotid Artery Stenosis1
2RecruitingDiagnosticMetastatic Hormone Refractory Prostate Cancer / Prostate Cancer / Prostate Neoplasms / Prostatic Neoplasms1
1CompletedDiagnosticMetastatic Hormone Refractory Prostate Cancer1
1RecruitingDiagnosticHormone-Resistant Prostate Cancer / Metastatic Hormone Refractory Prostate Cancer / Metastatic Malignant Neoplasm in the Bone1
1RecruitingDiagnosticProstate Cancer1
Not AvailableCompletedDiagnosticFluorocholine / Prostate Cancer1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Tablet0.25 mg
Injection, solutionIntravenous250 MBq/ml
InjectionIntravenous10 mCi/1mL
InjectionIntravenous600 mCi/1mL
InjectionIntravenous91.5 mCi/1mL
Injection, solutionIntravenous200 mCi/1mL
Injection, solutionIntravenous475 mCi/1mL
InjectionIntravenous200 mCi/1mL
InjectionIntravenous200 mg/1mL
Injection, solution250 MBq/ml
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
logP0.15ChemAxon
pKa (Strongest Acidic)3.17ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count0ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area0 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity0.87 m3·mol-1ChemAxon
Polarizability0.44 Å3ChemAxon
Number of Rings0ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Drug created on November 30, 2015 12:10 / Updated on June 12, 2020 10:52

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