flortaucipir F 18 ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
5396 1522051-90-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • flortaucipir F 18
  • flortaucipir (18F)
  • flortaucipir
  • flortaucipir F18
  • tauvid
  • 18F-AV-1451
  • [F-18]T807
  • LY3191748
Flortaucipir F 18 is a radioactive diagnostic agent indicated for positron emission tomography (PET) imaging of the brain to estimate the density and distribution of aggregated tau neurofibrillary tangles (NFTs) in adult patients with cognitive impairment who are being evaluated for Alzheimerโ€™s disease (AD). It binds to aggregated tau protein. In the brains of patients with AD, tau aggregates combine to form NFTs, one of two components required for the neuropathological diagnosis of AD. In vitro, flortaucipir F 18 binds to paired helical filament (PHF) tau purified from brain homogenates of donors with AD. The dissociation constant (Kd) of flortaucipir F 18 binding to PHFs is 0.57 nM. In vivo, flortaucipir F 18 is differentially retained in neocortical areas that contain aggregated tau. In vitro, tritiated flortaucipir has been reported to bind with low nanomolar affinity to monoamine oxidase-A and monoamine oxidase-B, which could contribute to off target binding
  • Molecular weight: 262.28
  • Formula: C16H10FN3
  • CLOGP: 3.18
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 1
  • TPSA: 41.57
  • ALOGS: -4.37
  • ROTB: 1

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
May 28, 2020 FDA AVID RADIOPHARMS INC

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC V09AX07 VARIOUS
DIAGNOSTIC RADIOPHARMACEUTICALS
CENTRAL NERVOUS SYSTEM
Other central nervous system diagnostic radiopharmaceuticals

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Positron emission tomography indication 82918005




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
30ML (8.1-51mCi/ML) TAUVID AVID RADIOPHARMS INC N212123 May 28, 2020 RX SOLUTION INTRAVENOUS May 28, 2025 NEW CHEMICAL ENTITY
50ML (8.1-51mCi/ML) TAUVID AVID RADIOPHARMS INC N212123 May 28, 2020 RX SOLUTION INTRAVENOUS May 28, 2025 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Microtubule-associated protein tau Structural BINDING AGENT Kd 9.24 DRUG LABEL DRUG LABEL

External reference:

IDSource
D11210 KEGG_DRUG
T1JP1KYU9O UNII
1415379-56-4 SECONDARY_CAS_RN
C4742689 UMLSCUI
CHEMBL3545253 ChEMBL_ID
70957463 PUBCHEM_CID
DB14914 DRUGBANK_ID
CHEMBL3546271 ChEMBL_ID
9100 IUPHAR_LIGAND_ID
DB15033 DRUGBANK_ID
018380 NDDF
878816002 SNOMEDCT_US
879808000 SNOMEDCT_US
4041601 VANDF
2372689 RXNORM
41402 MMSL
d10033 MMSL
10203 INN_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
TAUVID HUMAN PRESCRIPTION DRUG LABEL 1 0002-1210 INJECTION, SOLUTION 51 mCi INTRAVENOUS NDA 25 sections
TAUVID HUMAN PRESCRIPTION DRUG LABEL 1 0002-1210 INJECTION, SOLUTION 51 mCi INTRAVENOUS NDA 25 sections
TAUVID HUMAN PRESCRIPTION DRUG LABEL 1 0002-1220 INJECTION, SOLUTION 100 mCi INTRAVENOUS NDA 25 sections