Identification

Name
TAK-475
Accession Number
DB05317
Description

TAK-475 is a "squalene synthase inhibitor", a type of cholesterol-lowering drug that has not yet been brought to market.

Type
Small Molecule
Groups
Investigational
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Synonyms
Not Available

Pharmacology

Indication

Investigated for use/treatment in hyperlipidemia.

Contraindications & Blackbox Warnings
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Pharmacodynamics
Not Available
Mechanism of action

Squalene synthase inhibitors are believed to have potential advantages over statins, which inhibit 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase. HMG-CoA catalyzes the conversion of HMG-CoA to mevalonate and thus serves as the primary rate-limiting enzyme in the hepatic biosynthesis of cholesterol. Squalene synthase acts downstream of mevalonate, catalyzing the dimerization of farnesyl-pyrophosphate to squalene. This is the first step in the cholesterol biosynthetic pathway that is solely committed to the production of cholesterol, and researchers believe that blockade at this site may avoid the effects associated with decreased formation of isoprenolated intermediates and metabolites in the pathway beyond HMG-CoA reductase.

TargetActionsOrganism
USqualene synthaseNot AvailableHumans
U3-hydroxy-3-methylglutaryl-coenzyme A reductaseNot AvailableHumans
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
Affected organisms
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

Chemical Identifiers

UNII
Not Available
CAS number
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

References

General References
  1. Amano Y, Nishimoto T, Tozawa Ri, Ishikawa E, Imura Y, Sugiyama Y: Lipid-lowering effects of TAK-475, a squalene synthase inhibitor, in animal models of familial hypercholesterolemia. Eur J Pharmacol. 2003 Apr 11;466(1-2):155-61. [PubMed:12679152]
  2. Nishimoto T, Amano Y, Tozawa R, Ishikawa E, Imura Y, Yukimasa H, Sugiyama Y: Lipid-lowering properties of TAK-475, a squalene synthase inhibitor, in vivo and in vitro. Br J Pharmacol. 2003 Jul;139(5):911-8. [PubMed:12839864]
PubChem Substance
347910077

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3CompletedTreatmentDyslipidemia2
3CompletedTreatmentHigh Cholesterol6
3CompletedTreatmentType 2 Diabetes Mellitus1
3TerminatedTreatmentHigh Cholesterol4
2CompletedTreatmentHigh Cholesterol1
2CompletedTreatmentHyperlipidemias1
2TerminatedTreatmentHigh Cholesterol1

Pharmacoeconomics

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

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
Not Available
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Squalene synthase activity
Specific Function
Not Available
Gene Name
FDFT1
Uniprot ID
P37268
Uniprot Name
Squalene synthase
Molecular Weight
48114.87 Da
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Nadph binding
Specific Function
Transmembrane glycoprotein that is the rate-limiting enzyme in cholesterol biosynthesis as well as in the biosynthesis of nonsterol isoprenoids that are essential for normal cell function including...
Gene Name
HMGCR
Uniprot ID
P04035
Uniprot Name
3-hydroxy-3-methylglutaryl-coenzyme A reductase
Molecular Weight
97475.155 Da

Drug created on November 18, 2007 11:23 / Updated on June 12, 2020 10:52

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