NAV

CTS-21166

Identification

Generic Name
CTS-21166
DrugBank Accession Number
DB06073
Background

CTS-21166 is a small-molecule beta-secretase inhibitor, which is being developed as a disease-modifying treatment for Alzheimer's disease. CTS-21166 is the only BACE1 inhibitor that has passed Phase I clinical trial thus far. In 2008, CoMentis revealed this small compound as a transition-state analog inhibitor (structure is currently undisclosed) with excellent properties in brain penetration, selectivity, metabolic stability, and oral availability; all of these have met the requirements of an ideal oral drug candidate.

Type
Small Molecule
Groups
Investigational
Synonyms
Not Available

Pharmacology

Indication

Investigated for use/treatment in alzheimer's disease.

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Contraindications & Blackbox Warnings
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Pharmacodynamics

CTS-21166 produced a rapid and significant reduction of plasma amyloid beta, a key biomarker that is believed to be involved in the pathogenesis of Alzheimer's disease. CTS-21166 demonstrated excellent pharmacokinetic properties including dose proportional exposure and very low inter-subject pharmacokinetic variability.

Mechanism of action

Beta secretase is the enzyme thought responsible for causing Alzheimer’s. CTS-21166 is a highly selective, potent and orally active beta-secretase inhibitor.

TargetActionsOrganism
ABeta-secretase 1
inhibitor
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
Not Available
Classification
Not classified
Affected organisms
  • Humans and other mammals

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. Luo X, Yan R: Inhibition of BACE1 for therapeutic use in Alzheimer's disease. Int J Clin Exp Pathol. 2010 Jul 8;3(6):618-28. [Article]
PubChem Substance
347910328

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

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

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Details1. Beta-secretase 1
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Peptidase activity
Specific Function
Responsible for the proteolytic processing of the amyloid precursor protein (APP). Cleaves at the N-terminus of the A-beta peptide sequence, between residues 671 and 672 of APP, leads to the genera...
Gene Name
BACE1
Uniprot ID
P56817
Uniprot Name
Beta-secretase 1
Molecular Weight
55710.28 Da
References
  1. Albert JS: Progress in the development of beta-secretase inhibitors for Alzheimer's disease. Prog Med Chem. 2009;48:133-61. [Article]
  2. Panza F, Solfrizzi V, Frisardi V, Capurso C, D'Introno A, Colacicco AM, Vendemiale G, Capurso A, Imbimbo BP: Disease-modifying approach to the treatment of Alzheimer's disease: from alpha-secretase activators to gamma-secretase inhibitors and modulators. Drugs Aging. 2009;26(7):537-55. doi: 10.2165/11315770-000000000-00000. [Article]

Drug created at November 18, 2007 18:29 / Updated at June 12, 2020 16:52