REV131

Identification

Generic Name
REV131
DrugBank Accession Number
DB05032
Background

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.

Type
Small Molecule
Groups
Investigational
Synonyms
Not Available

Pharmacology

Indication

Investigated for use/treatment in allergic reaction, allergic rhinitis, and cataracts.

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Pharmacodynamics

Not Available

Mechanism of action

rEV131 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.

TargetActionsOrganism
UHistamine H4 receptorNot AvailableHumans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Approximately 8 hours

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
Not Available

Chemical Identifiers

UNII
V94JSH9V48
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
347909902

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2Unknown StatusNot AvailableOcular Inflammation1
1, 2Unknown StatusPreventionAllergy to Tree Pollen1

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
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 agoni...
Gene Name
HRH4
Uniprot ID
Q9H3N8
Uniprot Name
Histamine H4 receptor
Molecular Weight
44495.375 Da

Drug created at October 21, 2007 22:23 / Updated at June 12, 2020 16:52