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Flortaucipir

This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

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Identification

Generic Name
Flortaucipir
DrugBank Accession Number
DB15033
Background

Flortaucipir is under investigation in clinical trial NCT03507257 (Longitudinal Early-onset Alzheimer's Disease Study Protocol).

Type
Small Molecule
Groups
Investigational
Structure
3D
Similar Structures
Weight
Average: 263.275
Monoisotopic: 263.085875497
Chemical Formula
C16H10FN3
Synonyms
Not Available
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Pharmacology

Indication

Not Available

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Contraindications & Blackbox Warnings
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Pharmacodynamics

Not Available

Mechanism of action
TargetActionsOrganism
AMicrotubule-associated protein tau
modulator
Humans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

Not Available

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
Not Available

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
J09QS3Z3WB
CAS number
1415379-56-4
InChI Key
GETAAWDSFUCLBS-UHFFFAOYSA-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
IUPAC Name
2-fluoro-5-{5H-pyrido[4,3-b]indol-7-yl}pyridine
SMILES
FC1=CC=C(C=N1)C1=CC=C2C(NC3=C2C=NC=C3)=C1

References

General References
Not Available
ChemSpider
32699920
RxNav
2571858
ChEMBL
CHEMBL3546271
ZINC
ZINC000148048492
PDBe Ligand
S9C
PDB Entries
8byn

Clinical Trials

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PhaseStatusPurposeConditionsCountStart DateWhy Stopped100+ additional columns
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Not AvailableRecruitingNot AvailableAlzheimer's Disease (AD)1somestatusstop reasonjust information to hide
4Active Not RecruitingDiagnosticAlzheimer's Disease (AD)1somestatusstop reasonjust information to hide
4Enrolling by InvitationDiagnosticDementia With Lewy Body Disease1somestatusstop reasonjust information to hide
2CompletedDiagnosticAlzheimer's Disease (AD) / Decline, Cognitive1somestatusstop reasonjust information to hide
1Enrolling by InvitationBasic ScienceConcussion, Brain1somestatusstop reasonjust information to hide

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Not Available
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0111 mg/mLALOGPS
logP3.52ALOGPS
logP2.84Chemaxon
logS-4.4ALOGPS
pKa (Strongest Acidic)13.03Chemaxon
pKa (Strongest Basic)8.13Chemaxon
Physiological Charge1Chemaxon
Hydrogen Acceptor Count2Chemaxon
Hydrogen Donor Count1Chemaxon
Polar Surface Area41.57 Å2Chemaxon
Rotatable Bond Count1Chemaxon
Refractivity75.53 m3·mol-1Chemaxon
Polarizability27.23 Å3Chemaxon
Number of Rings4Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
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/MSsplash10-03di-0090000000-349b06e9830fc922d907
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-03di-0090000000-884968d45fb8216da218
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-03di-0090000000-1ae9cb2baae3a3b65d20
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-03di-0090000000-2d7bb1bd79ee2166e951
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-03di-0190000000-ad266ebf56afb1680e74
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-0frj-0190000000-b45e428e39b4af4db48d
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
Not Available

Targets

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Details1. Microtubule-associated protein tau
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Modulator
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
  1. Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]

Drug created at May 20, 2019 14:44 / Updated at August 27, 2024 19:16