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Identification
- Summary
Flortaucipir F-18 is a small lipophilic tracer containing [18F]fluoride capable of crossing the blood-brain barrier and binding to aggregated tau protein; used in PET imaging for the diagnosis of Alzheimer's disease.
- Generic Name
- Flortaucipir F-18
- DrugBank Accession Number
- DB14914
- Background
Flortaucipir F-18, also known as 18F-T807 and 18F-AV-1451, is a small indole molecule synthesized with a radioactive fluorine isotope.1 It is used as a marker in positron emission tomography (PET) imaging of patients suspected of having Alzheimer's disease. After crossing the blood-brain barrier, flortaucipir F-18 binds to aggregated tau protein, a hallmark of Alzheimer's disease whose incidence correlates well with disease progression.1,2,3
Although flortaucipir F-18 displays low levels of background binding throughout the brain,2 it does display off-target binding to monoamine oxidase MAO-A and MAO-B, as well as to regions containing high levels of melanin, neuromelanin, and iron.4,5. It was approved by the FDA on May 28, 2020, for sale by Avid Radiopharmaceuticals under the name TAUVID™ and is the first FDA-approved molecule for imaging aggregated tau protein in the brain.6
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Flortaucipir F-18 (DB14914)
- Weight
- Average: 262.278
Monoisotopic: 262.088410001 - Chemical Formula
- C16H10FN3
- Synonyms
- Flortaucipir (18F)
- Flortaucipir F 18
- External IDs
- (18F)AV 1451
- (F-18)T807
- 18F-AV-1451
- LY 3191748
- LY-3191748
- T-807 F-18
- T807 F-18
Pharmacology
- Indication
Flortaucipir F-18 is a radioactive agent indicated for positron emission tomography (PET) imaging of aggregated tau neurofibrillary tangles (NFTs) in adult patients under evaluation for Alzheimer's disease. Flortaucipir F-18 is not indicated for use in patients under evaluation for chronic traumatic encephalopathy.6
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Diagnostic agent Alzheimer's disease (ad) •••••••••••• ••••• ••••••••• - 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
Flortaucipir F-18 is a radioactive molecule that binds to and accumulates in tau NFT deposits allowing for imaging detection; however, non-specific binding and other factors allow for the possibility of misdiagnosis. As Flortaucipir F-18 is a radioactive substance, standard precautionary measures for protecting both patients and health care workers are advised. The safety and efficacy of flortaucipir F-18 in patients being evaluated for chronic traumatic encephalopathy are unknown and hence is not recommended.6
- Mechanism of action
Alzheimer's disease is a progressive neurodegenerative disease characterized by the build-up of hyperphosphorylated tau protein aggregates. Hyperphosphorylated tau forms dimers termed paired helical filaments (PHFs), which aggregate further to form neurofibrillary tangles (NFTs) associated with neurodegeneration and severity of Alzheimer's symptoms.1,2
Flortaucipir F-18 is a small molecule that contains radioactive 18F, which decays by positron emission to 18O with a half-life of 109.8 minutes.6 As a small relatively lipophilic molecule, flortaucipir F-18, following intravenous injection, quickly passes through systemic circulation, crosses the blood-brain barrier, and binds to NFTs. Once bound, the ensuing radioactive decay emits pairs of 511 keV gamma photons useful in diagnostic imaging. The pattern and intensity of emission during imaging is used in the diagnosis of Alzheimer's disease.2,6
Target Actions Organism AMicrotubule-associated protein tau binderHumans NAmine oxidase [flavin-containing] A binderHumans NAmine oxidase [flavin-containing] B binderHumans - Absorption
Flortaucipir F-18 is administered as an intravenous bolus injection, 6 and peak brain uptake in mice of 4.16% ID/g is achieved by 2 minutes.2 Fast transfer from the peripheral circulation to the brain was corroborated by human studies that demonstrated peak SUV in gray matter >2 across subjects approximately 5 minutes after administration.3
Pharmacokinetic studies in humans suggest that equilibrium is achieved by 55 minutes (Logan DVR) and by 80 - 100 minutes (SUVR),3 and current guidelines recommend initiating imaging approximately 80 minutes after initial administration.6
- Volume of distribution
Flortaucipir F-18 injected into mice accumulates primarily in the kidneys (14.99 ± 0.39 %ID/g at five minutes and 5.52 ± 0.91 %ID/g at 30 minutes post-injection) and liver (4.44 ± 0.16/5.99 ± 0.42 %ID/g at five/30 minutes, respectively). It is able to cross the blood-brain barrier, with relatively high penetration early (4.43 ± 0.91 %ID/g at five minutes) and low residual penetration later (0.62 ± 0.06 %ID/g at 30 minutes). Detectable amounts of Flortaucipir F-18 are found in the systemic circulation, as well as in muscle and bone.2
- Protein binding
Not Available
- Metabolism
Initial studies in mice described the parent compound and four uncharacterized metabolites, one of which, termed metabolite 1, is presumed to be [18F]fluoride. Plasma radioactivity corresponded only to the parent compound and metabolite 1. All metabolites were detected in the liver while all metabolites except metabolite 2 were found in the kidneys.2
- Route of elimination
The major route of elimination for Flortaucipir F-18 is via the kidneys.2
- Half-life
Flortaucipir F-18 plasma half-life was calculated at 17.0 ± 4.2 minutes; correction for metabolite half-life yielded a biexponential distribution with half-lives of 18.1 ± 5.8 and 2.4 ± 0.5 minutes.3
- Clearance
Not Available
- Adverse Effects
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Toxicity information regarding Flortaucipir F-18 is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as headaches and increased blood pressure. Symptomatic and supportive measures are recommended.
- 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
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 Tauvid Injection, solution 51 mCi/1mL Intravenous Eli Lilly Nederland B.V. 2020-05-28 2022-10-24 US 
Tauvid Injection, solution 100 mCi/1mL Intravenous Eli Lilly Nederland B.V. 2022-07-01 Not applicable US
Categories
- ATC Codes
- V09AX07 — Flortaucipir (18f)
- Drug Categories
- Classification
- Not classified
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- T1JP1KYU9O
- CAS number
- 1522051-90-6
- InChI Key
- GETAAWDSFUCLBS-SJPDSGJFSA-N
- InChI
- InChI=1S/C16H10FN3/c17-16-4-2-11(8-19-16)10-1-3-12-13-9-18-6-5-14(13)20-15(12)7-10/h1-9,20H/i17-1
- IUPAC Name
- 2-(¹⁸F)fluoro-5-{5H-pyrido[4,3-b]indol-7-yl}pyridine
- SMILES
- [18F]C1=CC=C(C=N1)C1=CC=C2C(NC3=C2C=NC=C3)=C1
References
- Synthesis Reference
Neil Vasdev, Timothy M. Shoup. "Radiosynthesis of tau radiopharmaceuticals." US patent US9546167B2, issued January 17, 2017.
- General References
- Wang YT, Edison P: Tau Imaging in Neurodegenerative Diseases Using Positron Emission Tomography. Curr Neurol Neurosci Rep. 2019 Jun 6;19(7):45. doi: 10.1007/s11910-019-0962-7. [Article]
- Xia CF, Arteaga J, Chen G, Gangadharmath U, Gomez LF, Kasi D, Lam C, Liang Q, Liu C, Mocharla VP, Mu F, Sinha A, Su H, Szardenings AK, Walsh JC, Wang E, Yu C, Zhang W, Zhao T, Kolb HC: [(18)F]T807, a novel tau positron emission tomography imaging agent for Alzheimer's disease. Alzheimers Dement. 2013 Nov;9(6):666-76. doi: 10.1016/j.jalz.2012.11.008. Epub 2013 Feb 12. [Article]
- Wooten DW, Guehl NJ, Verwer EE, Shoup TM, Yokell DL, Zubcevik N, Vasdev N, Zafonte RD, Johnson KA, El Fakhri G, Normandin MD: Pharmacokinetic Evaluation of the Tau PET Radiotracer (18)F-T807 ((18)F-AV-1451) in Human Subjects. J Nucl Med. 2017 Mar;58(3):484-491. doi: 10.2967/jnumed.115.170910. Epub 2016 Sep 22. [Article]
- Vermeiren C, Motte P, Viot D, Mairet-Coello G, Courade JP, Citron M, Mercier J, Hannestad J, Gillard M: The tau positron-emission tomography tracer AV-1451 binds with similar affinities to tau fibrils and monoamine oxidases. Mov Disord. 2018 Feb;33(2):273-281. doi: 10.1002/mds.27271. Epub 2017 Dec 26. [Article]
- Choi JY, Cho H, Ahn SJ, Lee JH, Ryu YH, Lee MS, Lyoo CH: Off-Target (18)F-AV-1451 Binding in the Basal Ganglia Correlates with Age-Related Iron Accumulation. J Nucl Med. 2018 Jan;59(1):117-120. doi: 10.2967/jnumed.117.195248. Epub 2017 Aug 3. [Article]
- FDA Approved Drug Products: Tauvid (flortaucipir F-18) injection [Link]
- External Links
- ChemSpider
- 32701063
- 2372689
- ChEMBL
- CHEMBL3545253
- Wikipedia
- Flortaucipir_(18F)
- FDA label
- Download (1.05 MB)
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 Alzheimer's Disease (AD) 1 somestatus stop reason just information to hide Not Available Completed Not Available Alzheimer's Disease (AD) / Early Mild Cognitive Impairment (EMCI) / Late Mild Cognitive Impairment (LMCI) / Mild Cognitive Impairment (MCI) / Significant Memory Concern (SMC) 1 somestatus stop reason just information to hide Not Available Completed Not Available Alzheimer's Disease (AD) / Human Immunodeficiency Virus (HIV) Infections 1 somestatus stop reason just information to hide Not Available Completed Not Available Alzheimer's Disease (AD) / Progressive Posterior Cortical Dysfunction (PPCD) 1 somestatus stop reason just information to hide Not Available Completed Not Available 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 Intravenous 100 mCi/1mL Injection, solution Intravenous 51 mCi/1mL - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8932557 No 2015-01-13 2029-05-19 US
Properties
- State
- Not Available
- Experimental Properties
Property Value Source logP 1.67 Xia et al 2013 - Predicted Properties
Property Value Source Water Solubility 0.0111 mg/mL ALOGPS logP 3.52 ALOGPS logP 2.84 Chemaxon logS -4.4 ALOGPS pKa (Strongest Acidic) 13.03 Chemaxon pKa (Strongest Basic) 8.13 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 41.57 Å2 Chemaxon Rotatable Bond Count 1 Chemaxon Refractivity 75.53 m3·mol-1 Chemaxon Polarizability 27.23 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-03di-0090000000-349b06e9830fc922d907 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-03di-0090000000-884968d45fb8216da218 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-03di-0090000000-2d7bb1bd79ee2166e951 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-03di-0090000000-1ae9cb2baae3a3b65d20 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0frj-0190000000-b45e428e39b4af4db48d Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-03di-0190000000-ad266ebf56afb1680e74 Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Binder
- Curator comments
- Flortaucipir F-18 binds to aggregated tau proteins including paired helical filaments (PHFs) with a Kd of 0.57 nM.
- General Function
- Promotes microtubule assembly and stability, and might be involved in the establishment and maintenance of neuronal polarity (PubMed:21985311). The C-terminus binds axonal microtubules while the N-terminus binds neural plasma membrane components, suggesting that tau functions as a linker protein between both (PubMed:21985311, PubMed:32961270). Axonal polarity is predetermined by TAU/MAPT localization (in the neuronal cell) in the domain of the cell body defined by the centrosome. The short isoforms allow plasticity of the cytoskeleton whereas the longer isoforms may preferentially play a role in its stabilization
- Specific Function
- actin binding
- Gene Name
- MAPT
- Uniprot ID
- P10636
- Uniprot Name
- Microtubule-associated protein tau
- Molecular Weight
- 78927.025 Da
References
- Wang YT, Edison P: Tau Imaging in Neurodegenerative Diseases Using Positron Emission Tomography. Curr Neurol Neurosci Rep. 2019 Jun 6;19(7):45. doi: 10.1007/s11910-019-0962-7. [Article]
- Xia CF, Arteaga J, Chen G, Gangadharmath U, Gomez LF, Kasi D, Lam C, Liang Q, Liu C, Mocharla VP, Mu F, Sinha A, Su H, Szardenings AK, Walsh JC, Wang E, Yu C, Zhang W, Zhao T, Kolb HC: [(18)F]T807, a novel tau positron emission tomography imaging agent for Alzheimer's disease. Alzheimers Dement. 2013 Nov;9(6):666-76. doi: 10.1016/j.jalz.2012.11.008. Epub 2013 Feb 12. [Article]
- Wooten DW, Guehl NJ, Verwer EE, Shoup TM, Yokell DL, Zubcevik N, Vasdev N, Zafonte RD, Johnson KA, El Fakhri G, Normandin MD: Pharmacokinetic Evaluation of the Tau PET Radiotracer (18)F-T807 ((18)F-AV-1451) in Human Subjects. J Nucl Med. 2017 Mar;58(3):484-491. doi: 10.2967/jnumed.115.170910. Epub 2016 Sep 22. [Article]
- Vermeiren C, Motte P, Viot D, Mairet-Coello G, Courade JP, Citron M, Mercier J, Hannestad J, Gillard M: The tau positron-emission tomography tracer AV-1451 binds with similar affinities to tau fibrils and monoamine oxidases. Mov Disord. 2018 Feb;33(2):273-281. doi: 10.1002/mds.27271. Epub 2017 Dec 26. [Article]
- FDA Approved Drug Products: Tauvid (flortaucipir F-18) injection [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Binder
- General Function
- Catalyzes the oxidative deamination of primary and some secondary amine such as neurotransmitters, with concomitant reduction of oxygen to hydrogen peroxide and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues (PubMed:18391214, PubMed:20493079, PubMed:24169519, PubMed:8316221). Preferentially oxidizes serotonin (PubMed:20493079, PubMed:24169519). Also catalyzes the oxidative deamination of kynuramine to 3-(2-aminophenyl)-3-oxopropanal that can spontaneously condense to 4-hydroxyquinoline (By similarity)
- Specific Function
- aliphatic amine oxidase activity
- Gene Name
- MAOA
- Uniprot ID
- P21397
- Uniprot Name
- Amine oxidase [flavin-containing] A
- Molecular Weight
- 59681.27 Da
References
- Vermeiren C, Motte P, Viot D, Mairet-Coello G, Courade JP, Citron M, Mercier J, Hannestad J, Gillard M: The tau positron-emission tomography tracer AV-1451 binds with similar affinities to tau fibrils and monoamine oxidases. Mov Disord. 2018 Feb;33(2):273-281. doi: 10.1002/mds.27271. Epub 2017 Dec 26. [Article]
- FDA Approved Drug Products: Tauvid (flortaucipir F-18) injection [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Binder
- General Function
- Catalyzes the oxidative deamination of primary and some secondary amines such as neurotransmitters, and exogenous amines including the tertiary amine, neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), with concomitant reduction of oxygen to hydrogen peroxide and participates in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues (PubMed:11049757, PubMed:11134050, PubMed:20493079, PubMed:8316221, PubMed:8665924). Preferentially degrades benzylamine and phenylethylamine (PubMed:11049757, PubMed:11134050, PubMed:20493079, PubMed:8316221, PubMed:8665924)
- Specific Function
- aliphatic amine oxidase activity
- Gene Name
- MAOB
- Uniprot ID
- P27338
- Uniprot Name
- Amine oxidase [flavin-containing] B
- Molecular Weight
- 58762.475 Da
References
- Vermeiren C, Motte P, Viot D, Mairet-Coello G, Courade JP, Citron M, Mercier J, Hannestad J, Gillard M: The tau positron-emission tomography tracer AV-1451 binds with similar affinities to tau fibrils and monoamine oxidases. Mov Disord. 2018 Feb;33(2):273-281. doi: 10.1002/mds.27271. Epub 2017 Dec 26. [Article]
- FDA Approved Drug Products: Tauvid (flortaucipir F-18) injection [Link]
Drug created at May 20, 2019 14:34 / Updated at October 06, 2020 17:43