AM103

Identification

Generic Name
AM103
DrugBank Accession Number
DB05225
Background

AM103 is a novel inhibitor of 5-lipoxygenase-activiting protein (FLAP) that has demonstrated potential to treat asthma and cardiovascular disease by preventing the synthesis of LT, which triggers inflammation. It is being developed by Amira.

Type
Small Molecule
Groups
Investigational
Synonyms
Not Available

Pharmacology

Indication

For the treatment of asthma and cardiovascular disease.

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Contraindications & Blackbox Warnings
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Pharmacodynamics

Results from the Phase I trial show that AM103 is safe and well-tolerated at doses up to 1,000 mg per day with no evidence of significant side effects. Pharmacodynamic data demonstrated a robust and statistically significant reduction of LTB4 and LTE4 in a dose-dependent manner.

Mechanism of action

The exact mechanism of actions is not known, however, AM103 inhibits the 5-lipoxygenase-activiting protein (FLAP). This prevents the synthesis of LT, which normally triggers inflammation.

TargetActionsOrganism
UArachidonate 5-lipoxygenase-activating protein
inhibitor
Humans
Absorption

Well absorbed orally.

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
  • 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
Not Available
PubChem Substance
347910035

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
Chromatographic Properties
Collision Cross Sections (CCS)
Not Available

Targets

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Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Protein n-terminus binding
Specific Function
Required for leukotriene biosynthesis by ALOX5 (5-lipoxygenase). Anchors ALOX5 to the membrane. Binds arachidonic acid, and could play an essential role in the transfer of arachidonic acid to ALOX5...
Gene Name
ALOX5AP
Uniprot ID
P20292
Uniprot Name
Arachidonate 5-lipoxygenase-activating protein
Molecular Weight
18156.96 Da
References
  1. Sampson AP: FLAP inhibitors for the treatment of inflammatory diseases. Curr Opin Investig Drugs. 2009 Nov;10(11):1163-72. [Article]

Drug created at October 21, 2007 22:24 / Updated at May 05, 2022 16:38