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Identification
NameREV131
Accession NumberDB05032
TypeSmall Molecule
GroupsInvestigational
Description

rEV131 is in development for allergic rhinitis, asthma and several inflammatory eye diseases. It is a topically delivered small protein that acts as an anti-inflammatory agent.

Structure
Thumb
SynonymsNot Available
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
CategoriesNot Available
UNIINot Available
CAS numberNot Available
WeightNot Available
Chemical FormulaNot Available
InChI KeyNot Available
InChINot Available
IUPAC NameNot Available
SMILESNot Available
Taxonomy
ClassificationNot classified
Pharmacology
IndicationInvestigated for use/treatment in allergic reaction, allergic rhinitis, and cataracts.
PharmacodynamicsNot Available
Mechanism of actionrEV131 is smaller than therapeutic antibodies and its compact structure gives good bioavailablity by a number of routes including: injected, inhaled, intraperitoneal, topical (ocular and nasal). The molecule is thermo-stable and can be stored in solution for more than 18 months at room temperature without significant loss of activity. This is an attractive feature for a protein drug candidate. rEV131 is a novel histamine binding protein that modulates the immediate inflammatory response largely caused by the release of pre-formed histamine from mast cells in the skin. This molecule binds histamine at two active sites, one of which has an affinity for histamine 10 - 100 times higher than any known histamine receptor. This enables rEV131 to out compete the body's natural receptors and prevent histamine from reaching and activating them. There are at least four different natural histamine receptors. The most recently discovered H4 receptor, was described in 2001, and appears to be involved in the late phase inflammatory process. rEV131 is understood to be the only drug candidate in clinical development, which prevents activation of the H4 receptor. rEV131 has demonstrated activity against both early and late phase inflammation in clinical and preclinical studies. This differentiates it from approved treatments: anti-histamines used in early phase inflammation and corticosteroid therapies, which are used predominantly in late phase inflammation. A favourable safety profile and a variety of delivery routes provide additional potential advantages for rEV131 over existing therapies.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeApproximately 8 hours
ClearanceNot Available
ToxicityNot Available
Affected organismsNot Available
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal AbsorptionNot AvailableNot Available
Blood Brain BarrierNot AvailableNot Available
Caco-2 permeableNot AvailableNot Available
P-glycoprotein substrateNot AvailableNot Available
P-glycoprotein inhibitor INot AvailableNot Available
P-glycoprotein inhibitor IINot AvailableNot Available
Renal organic cation transporterNot AvailableNot Available
CYP450 2C9 substrateNot AvailableNot Available
CYP450 2D6 substrateNot AvailableNot Available
CYP450 3A4 substrateNot AvailableNot Available
CYP450 1A2 substrateNot AvailableNot Available
CYP450 2C9 inhibitorNot AvailableNot Available
CYP450 2D6 inhibitorNot AvailableNot Available
CYP450 2C19 inhibitorNot AvailableNot Available
CYP450 3A4 inhibitorNot AvailableNot Available
CYP450 inhibitory promiscuityNot AvailableNot Available
Ames testNot AvailableNot Available
CarcinogenicityNot AvailableNot Available
BiodegradationNot AvailableNot Available
Rat acute toxicityNot AvailableNot applicable
hERG inhibition (predictor I)Not AvailableNot Available
hERG inhibition (predictor II)Not AvailableNot Available
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot Available
Predicted PropertiesNot Available
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesNot Available
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug InteractionsNot Available
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Histamine receptor activity
Specific Function:
The H4 subclass of histamine receptors could mediate the histamine signals in peripheral tissues. Displays a significant level of constitutive activity (spontaneous activity in the absence of agonist).
Gene Name:
HRH4
Uniprot ID:
Q9H3N8
Molecular Weight:
44495.375 Da
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Drug created on October 21, 2007 16:23 / Updated on September 13, 2013 11:58