flortaucipir F 18 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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 Alzheimer’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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 3.254 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 1.493 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 34.514 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 18.113 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 7.130 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 21.440 % High 1
herg hERG pIC50 5.900 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 3.350 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 26.792 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 6.530 % High 1
kinase-safety-class AAK1,ACVR1B,ACVR2A,ACVR2B,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BRAF,CAMK2A,CAMK2B,CAMK2D,CAMK2G,CDK1,CDK14,CDK16,CDK19,CDK2,CDK3,CDK4,CDK5,CDK6,CDK7,CDK8,CDK9,CHEK1,CLK2,CLK4,CSF1R,CSNK1A1,CSNK1A1L,CSNK1D,CSNK1E,CSNK1G1,CSNK1G2,CSNK1G3,CSNK2A1,CSNK2A3,DDR1,DYRK1A,DYRK1B,DYRK2,DYRK3,EGFR,EIF2AK3,ERBB2,FLT3,GAK,GRK1,GRK2,GRK3,GSK3A,GSK3B,HASPIN,IKBKB,INSR,IRAK1,IRAK3,IRAK4,ITK,JAK1,JAK2,JAK3,KDR,KIT,LCK,LRRK2,MAP2K1,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K21,MAP3K7,MAP3K9,MAP4K1,MAP4K2,MAP4K3,MAP4K4,MAP4K5,MAPK1,MAPK10,MAPK12,MAPK3,MAPK7,MAPK9,MARK1,MARK2,MARK3,MARK4,MELK,MET,MINK1,MKNK1,MKNK2,MTOR,NTRK1,NTRK2,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM2,PRKAA1,PRKAA2,PRKCD,PRKCZ,PRKD1,PRKDC,ROCK1,ROCK2,SGK1,SIK2,SIK3,SRC,STK10,STK17A,STK33,SYK,TEK,TGFBR1,TNIK,TTK,ULK1,ULK2 131
kinase-selectivity-class ACVR1B,ACVR2A,ACVR2B,AURKB,AURKC,CAMK2B,CAMK2D,CDK1,CDK8,CDK9,CHUK,CLK2,CLK4,DYRK1A,DYRK1B,DYRK2,DYRK3,EGFR,ERBB2,GRK2,GSK3A,GSK3B,HASPIN,HIPK2,IKBKB,IRAK1,IRAK3,IRAK4,LCK,MAP3K10,MAP3K21,MAP4K1,MAP4K3,MAP4K4,MAP4K5,MARK1,MARK2,MARK3,MARK4,MINK1,MKNK1,MKNK2,PDK1,PIK3CA,PIK3CD,PIK3CG,PIM3,PRKAA1,PRKDC,RIPK3,ROCK1,ROCK2,SGK1,SIK2,SIK3,STK17A,TGFBR1,TNIK,ULK1 59
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 5.649 High 1
mh-clint Mouse hepatocyte intrinsic clearance 21.677 High 1
mppb Mouse plasma protein binding (% unbound) 5.630 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 3.873 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 14.370 % High 1
rh-clint Rat hepatocyte intrinsic clearance 11.885 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 17.150 % High 1
rppb Rat plasma protein binding (% unbound) 4.160 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 4.093 uM High 1

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

Related Drugs by ATC class:

V09AX Other central nervous system diagnostic radiopharmaceuticals 3 drugs
florbetaben F18Florbetapir F-18Flutemetamol (18F)

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

DiseaseRelationSNOMED_IDDOID
Positron emission tomography indication 82918005




🐶 Veterinary Drug Use

None

🐶 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)

None

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
4041601 VANDF
C4742689 UMLSCUI
CHEBI:755541 CHEBI
CHEMBL3545253 ChEMBL_ID
70957463 PUBCHEM_CID
DB14914 DRUGBANK_ID
CHEMBL3546271 ChEMBL_ID
10203 INN_ID
DB15033 DRUGBANK_ID
878816002 SNOMEDCT_US
879808000 SNOMEDCT_US
366398 MMSL
41402 MMSL
d10033 MMSL
018380 NDDF
9100 IUPHAR_LIGAND_ID
2372689 RXNORM
T1JP1KYU9O INXIGHT DRUGS

Pharmaceutical products:

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