Elafin
Identification
- Generic Name
- Elafin
- DrugBank Accession Number
- DB05161
- Background
Elafin is a human protein that is produced naturally in the skin, lung and breast, protecting the respective tissue from destruction by the immune system. Elafin’s ability to block the activity of destructive enzymes that are involved in inflammatory reactions makes it a highly promising active compound for the treatment of inflammatory lung diseases or severe reperfusion injuries occurring after heart attacks, serious injuries and organ transplantation. The excellent tolerability of Elafin in human subjects was demonstrated in a Phase I clinical single dose escalating study.
- Type
- Small Molecule
- Groups
- Investigational
- Synonyms
- Not Available
Pharmacology
- Indication
Investigated for use/treatment in inflammatory disorders (unspecified).
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- Pharmacodynamics
Not Available
- Mechanism of action
Elafin is able to abrogate lipopolysaccharide-induced production of monocyte chemotactic protein 1 in monocytes by inhibiting AP-1 and NFkappaB activation. Due to its selective expression at mucosal surfaces as well as in alveolar macrophages, monocytes and neutrophils, the ability of Elafin to inhibit the lipopolysaccharide signaling pathway may be important in disease states such as cystic fibrosis, pneumonia, and acute respiratory distress syndrome. The inhibition of two key inflammatory pathways confirms the importance of Elafin as a mediator of the innate immune response.
Target Actions Organism UNeutrophil elastase Not Available Humans UMyeloblastin 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
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- 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
- Not Available
- CAS number
- Not Available
- InChI Key
- Not Available
- InChI
- Not Available
- IUPAC Name
- Not Available
- SMILES
- Not Available
References
Clinical Trials
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Phase Status Purpose Conditions Count 1 Completed Treatment Pulmonary Arterial Hypertension (PAH) 1
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
- Serine-type endopeptidase activity
- Specific Function
- Modifies the functions of natural killer cells, monocytes and granulocytes. Inhibits C5a-dependent neutrophil enzyme release and chemotaxis.
- Gene Name
- ELANE
- Uniprot ID
- P08246
- Uniprot Name
- Neutrophil elastase
- Molecular Weight
- 28517.81 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Serine-type peptidase activity
- Specific Function
- Polymorphonuclear leukocyte serine protease that degrades elastin, fibronectin, laminin, vitronectin, and collagen types I, III, and IV (in vitro) and causes emphysema when administered by tracheal...
- Gene Name
- PRTN3
- Uniprot ID
- P24158
- Uniprot Name
- Myeloblastin
- Molecular Weight
- 27806.815 Da
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Peroxidase activity
- Specific Function
- Part of the host defense system of polymorphonuclear leukocytes. It is responsible for microbicidal activity against a wide range of organisms. In the stimulated PMN, MPO catalyzes the production o...
- Gene Name
- MPO
- Uniprot ID
- P05164
- Uniprot Name
- Myeloperoxidase
- Molecular Weight
- 83867.71 Da
References
- Tiefenbacher CP, Ebert M, Niroomand F, Batkai S, Tillmanns H, Zimmermann R, Kubler W: Inhibition of elastase improves myocardial function after repetitive ischaemia and myocardial infarction in the rat heart. Pflugers Arch. 1997 Mar;433(5):563-70. [Article]
Drug created at October 21, 2007 22:23 / Updated at June 12, 2020 16:52