Flutemetamol (18F) 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
4301 765922-62-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • Flutemetamol (18F)
  • 18F-Flutemetamol
  • flutemetamol F 18 injection
  • flutemetamol F 18
  • vizamyl
  • flutemetamol F18
  • flutemetamol F-18
used for PET imaging of brain fibrillar amyloid beta
  • Molecular weight: 273.32
  • Formula: C14H11FN2OS
  • CLOGP: 4.30
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 2
  • TPSA: 45.15
  • ALOGS: -4.31
  • ROTB: 2

  • Status: OFP

  • 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 4.077 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.817 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 37.154 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 146.893 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 0.690 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 1.360 % High 1
herg hERG pIC50 4.488 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 812.831 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 61.802 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 0.720 % High 1
kinase-safety-class ACVR1B,ACVR2A,ACVR2B,ACVRL1,AKT2,AKT3,ALK,AURKA,AURKB,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK1,CDK2,CDK5,CDK9,CHEK1,CLK4,CSF1R,DDR1,DYRK1A,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,IKBKB,IRAK1,ITK,JAK1,JAK2,KDR,KIT,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK10,MAPK7,MAPK9,MAPKAPK2,MARK4,MELK,MET,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM1,PIM2,PRKAA1,PRKCD,PRKDC,SGK1,SIK2,SIK3,STK10,STK33,SYK,TEK,TGFBR1,TNIK,TTK,UHMK1,ULK1,ULK2,ZAP70 83
kinase-selectivity-class ACVR2A,ACVR2B,BRAF,CAMK2D,DYRK1B,GRK2,MAP2K6,MAP3K21,MAPK7,PDK4,PIK3CA,PIK3CB,PIK3CD,PRKDC,SIK2,SIK3,STK33,TTK,ULK1 19
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 6.577 High 1
mh-clint Mouse hepatocyte intrinsic clearance 202.302 High 1
mppb Mouse plasma protein binding (% unbound) 1.610 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 1.294 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 3.180 % High 1
rh-clint Rat hepatocyte intrinsic clearance 271.644 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 15.820 % High 1
rppb Rat plasma protein binding (% unbound) 0.780 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 0.575 uM High 1

Approvals:

DateAgencyCompanyOrphan
Sept. 27, 2017 PMDA Nihon Medi-Physics Co Ltd
Oct. 25, 2013 FDA GE HEALTHCARE
Aug. 22, 2014 EMA GE Healthcare AS

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Flushing 576.36 98.90 133 595 88358 90539361
Dyspnoea 137.75 98.90 85 643 880870 89746849
Back pain 124.79 98.90 57 671 317118 90310601
Chest discomfort 116.53 98.90 43 685 138322 90489397

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Flushing 155.60 91.27 34 132 36994 42584175

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Flushing 667.59 117.17 152 659 104584 110483904
Back pain 176.40 117.17 74 737 370922 110217566
Dyspnoea 138.97 117.17 90 721 1106782 109481706

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC V09AX04 VARIOUS
DIAGNOSTIC RADIOPHARMACEUTICALS
CENTRAL NERVOUS SYSTEM
Other central nervous system diagnostic radiopharmaceuticals
FDA MoA N0000000205 Radiopharmaceutical Activity
MeSH PA D003287 Contrast Media
MeSH PA D007202 Indicators and Reagents
MeSH PA D019275 Radiopharmaceuticals
MeSH PA D064907 Diagnostic Uses of Chemicals
FDA EPC N0000177914 Radioactive Diagnostic Agent
CHEBI has role CHEBI:37336 radioactive imaging agent

Related Drugs by ATC class:

V09AX Other central nervous system diagnostic radiopharmaceuticals 3 drugs

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

DiseaseRelationSNOMED_IDDOID
Positron emission tomography indication 82918005
Diagnosis of Alzheimer's disease indication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.2 acidic
pKa2 3.58 Basic
pKa3 2.7 Basic

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
Amyloid beta A4 protein Membrane other Ki 9.15 CHEMBL

External reference:

IDSource
D10231 KEGG_DRUG
4038255 VANDF
C2983948 UMLSCUI
CHEMBL2042122 ChEMBL_ID
DB09151 DRUGBANK_ID
15950376 PUBCHEM_CID
1486025 RXNORM
206870 MMSL
29778 MMSL
d08135 MMSL
016452 NDDF
456996004 SNOMEDCT_US
456997008 SNOMEDCT_US
CHEBI:76611 CHEBI
9169 INN_ID
C581552 MESH_SUPPLEMENTAL_RECORD_UI
L49M066S0O UNII

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Vizamyl HUMAN PRESCRIPTION DRUG LABEL 1 17156-067 SOLUTION 4.05 mCi INTRAVENOUS NDA 28 sections
Vizamyl HUMAN PRESCRIPTION DRUG LABEL 1 17156-067 SOLUTION 4.05 mCi INTRAVENOUS NDA 28 sections