DG031
Identification
- Generic Name
- DG031
- DrugBank Accession Number
- DB04929
- Background
DG031, deCODE genetics's lead compound, is being developed for the prevention of myocardial infarction, or heart attack.
- Type
- Small Molecule
- Groups
- Investigational
- Synonyms
- Not Available
Pharmacology
- Indication
Investigated for use/treatment in heart disease and myocardial infarction.
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- Pharmacodynamics
DG031 is an inhibitor of 5-lipoxygenase activating protein, or FLAP. deCODE has linked variants in the gene encoding FLAP, and the gene encoding leukotriene A4 hydrolase (LTA4H) to risk of heart attack. These variants appear to confer increased risk of heart attack by increasing the production of leukotriene B4 (LTB4), a potent driver of inflammation produced in atherosclerotic plaques. In Phase II trials completed last year, DG031 was shown to be well tolerated at all doses tested and to reduce the production of LTB4 in a dose-dependent manner. Late last year deCODE discovered that the HapK variant of the LTA4H gene, discovered in Iceland and which confers a moderate increase in risk of heart attack in people of predominantly European ancestry, confers a 250% increase in risk of the disease in African Americans. deCODE licensed DG031 from Bayer AG, which developed it originally for the treatment of asthma. In deCODE’s clinical trials and those conducted previously by Bayer, a total of approximately 2000 people have been dosed with DG031.
- Mechanism of action
DG031 inhibits the activity of the FLAP, or 5-lipoxygenase activating protein, that modulates the activity of the leukotriene pathway.
Target Actions Organism UArachidonate 5-lipoxygenase-activating protein Not Available 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
- Not Available
- External Links
- PubChem Substance
- 347909852
Clinical Trials
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
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- 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
Drug created at October 21, 2007 22:23 / Updated at June 12, 2020 16:52