Identification

Name
Elafin
Accession Number
DB05161
Type
Small Molecule
Groups
Investigational
Description

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.

Synonyms
Not Available
Categories
UNII
Not Available
CAS number
Not Available
Weight
Not Available
Chemical Formula
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

Pharmacology

Indication

Investigated for use/treatment in inflammatory disorders (unspecified).

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.

TargetActionsOrganism
UNeutrophil elastaseNot AvailableHuman
UMyeloblastinNot AvailableHuman
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
Toxicity
Not Available
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AbacavirThe serum concentration of Abacavir can be decreased when it is combined with Elafin.Approved, Investigational
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Elafin.Approved, Investigational
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Elafin.Approved, Illicit, Investigational
Ambroxol acefyllinateThe serum concentration of Ambroxol acefyllinate can be decreased when it is combined with Elafin.Experimental, Investigational
AmineptineThe serum concentration of Amineptine can be increased when it is combined with Elafin.Illicit, Withdrawn
AminophyllineThe serum concentration of Aminophylline can be decreased when it is combined with Elafin.Approved
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Elafin.Approved
AmitriptylinoxideThe serum concentration of Amitriptylinoxide can be increased when it is combined with Elafin.Approved, Investigational
AmoxapineThe serum concentration of Amoxapine can be increased when it is combined with Elafin.Approved
BoceprevirThe serum concentration of Elafin can be decreased when it is combined with Boceprevir.Approved, Withdrawn
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Elafin.Approved, Investigational
ButriptylineThe serum concentration of Butriptyline can be increased when it is combined with Elafin.Approved
CabergolineThe serum concentration of Cabergoline can be increased when it is combined with Elafin.Approved
CarbamazepineThe metabolism of Elafin can be increased when combined with Carbamazepine.Approved, Investigational
ClarithromycinThe therapeutic efficacy of Clarithromycin can be decreased when used in combination with Elafin.Approved
ClomipramineThe serum concentration of Clomipramine can be increased when it is combined with Elafin.Approved, Investigational, Vet Approved
CyclophosphamideThe risk or severity of adverse effects can be increased when Elafin is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Elafin.Approved, Investigational, Vet Approved
DelavirdineThe serum concentration of Delavirdine can be decreased when it is combined with Elafin.Approved
DesipramineThe serum concentration of Desipramine can be increased when it is combined with Elafin.Approved, Investigational
DibenzepinThe serum concentration of Dibenzepin can be increased when it is combined with Elafin.Experimental
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be decreased when it is combined with Elafin.Approved, Investigational
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Elafin.Approved
DihydroergotamineThe serum concentration of Dihydroergotamine can be increased when it is combined with Elafin.Approved, Investigational
DiltiazemThe metabolism of Diltiazem can be decreased when combined with Elafin.Approved, Investigational
DimetacrineThe serum concentration of Dimetacrine can be increased when it is combined with Elafin.Approved, Withdrawn
DosulepinThe serum concentration of Dosulepin can be increased when it is combined with Elafin.Approved
DoxepinThe serum concentration of Doxepin can be increased when it is combined with Elafin.Approved, Investigational
DyphyllineThe serum concentration of Dyphylline can be decreased when it is combined with Elafin.Approved
EnfuvirtideThe serum concentration of Enfuvirtide can be increased when it is combined with Elafin.Approved, Investigational
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Elafin.Approved
ErgonovineThe serum concentration of Ergonovine can be increased when it is combined with Elafin.Approved
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Elafin.Approved
EstradiolThe serum concentration of Estradiol can be decreased when it is combined with Elafin.Approved, Investigational, Vet Approved
Estradiol cypionateThe serum concentration of Estradiol cypionate can be decreased when it is combined with Elafin.Approved, Investigational, Vet Approved
Estradiol valerateThe serum concentration of Estradiol valerate can be decreased when it is combined with Elafin.Approved, Investigational, Vet Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be decreased when it is combined with Elafin.Approved
EtravirineThe serum concentration of Etravirine can be decreased when it is combined with Elafin.Approved
GarlicThe serum concentration of Elafin can be decreased when it is combined with Garlic.Approved, Nutraceutical
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Elafin.Approved
IprindoleThe serum concentration of Iprindole can be increased when it is combined with Elafin.Experimental
LofepramineThe serum concentration of Lofepramine can be increased when it is combined with Elafin.Experimental
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Elafin.Approved, Investigational
MelitracenThe serum concentration of Melitracen can be increased when it is combined with Elafin.Experimental, Investigational
MestranolThe serum concentration of Mestranol can be decreased when it is combined with Elafin.Approved
MethylergometrineThe serum concentration of Methylergometrine can be increased when it is combined with Elafin.Approved
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Elafin.Approved, Illicit
NefazodoneThe serum concentration of Nefazodone can be increased when it is combined with Elafin.Approved, Withdrawn
NortriptylineThe serum concentration of Nortriptyline can be increased when it is combined with Elafin.Approved
OpipramolThe serum concentration of Opipramol can be increased when it is combined with Elafin.Investigational
PethidineThe risk or severity of adverse effects can be increased when Elafin is combined with Pethidine.Approved
ProtriptylineThe serum concentration of Protriptyline can be increased when it is combined with Elafin.Approved
RiociguatThe serum concentration of Riociguat can be increased when it is combined with Elafin.Approved
SildenafilThe serum concentration of Sildenafil can be increased when it is combined with Elafin.Approved, Investigational
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Elafin.Approved
St. John's WortThe metabolism of Elafin can be increased when combined with St. John's Wort.Approved, Investigational, Nutraceutical
TacrolimusThe metabolism of Tacrolimus can be decreased when combined with Elafin.Approved, Investigational
TemsirolimusThe risk or severity of adverse effects can be increased when Elafin is combined with Temsirolimus.Approved
TheophyllineThe serum concentration of Theophylline can be decreased when it is combined with Elafin.Approved
TianeptineThe serum concentration of Tianeptine can be increased when it is combined with Elafin.Approved, Investigational
TipranavirThe serum concentration of Elafin can be decreased when it is combined with Tipranavir.Approved, Investigational
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Elafin.Approved, Investigational
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Elafin.Approved
Valproic AcidThe serum concentration of Valproic Acid can be decreased when it is combined with Elafin.Approved, Investigational
VerapamilThe metabolism of Verapamil can be decreased when combined with Elafin.Approved
ZidovudineThe serum concentration of Zidovudine can be decreased when it is combined with Elafin.Approved
Food Interactions
Not Available

References

General References
Not Available
External Links
PubChem Substance
347909990
Wikipedia
Elafin

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Not Yet RecruitingTreatmentPulmonary 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

Taxonomy

Classification
Not classified

Targets

Kind
Protein
Organism
Human
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
Human
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
Human
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
  1. 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. [PubMed:9049140]

Drug created on October 21, 2007 16:23 / Updated on June 02, 2018 07:37