Explore a selection of our essential drug information below, or:
Identification
- Generic Name
- JSM 6427
- DrugBank Accession Number
- DB06139
- Background
JSM 6427 is the first small molecule alpha5beta1 integrin receptor antagonist of its kind to be developed. It has been biologically validated for therapeutic use in the prevention and treatment of wet AMD, the leading cause of blindness in people over the age of 55.
- Type
- Small Molecule
- Groups
- Investigational
- Synonyms
- Not Available
Pharmacology
- Indication
Investigated for use/treatment in macular degeneration.
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The integrin α5β1 is expressed on several types of inflammatory cells and mediates the migration of these cells into the inflamed tissue. By administering JSM-6427, the infiltration of inflammatory cells into the inflamed tissue will be inhibited and thus inflammation suppressed as shown in models of peritonitis and retinal inflammation.
- Mechanism of action
Wet AMD causes vision loss due to abnormal growth of new blood vessels in the choriocapillaris. New blood vessels arise as a result of proliferation, migration and differentiation of pre-existing blood vessel cells (endothelium). In order for the endothelium to form functional new blood vessels, they make use of cell surface adhesion receptors called integrins. These molecules are critical for the interaction between a vascular endothelial cell and its surrounding environment. The disruption of the integrin receptor represents a new therapeutic approach for the treatment of AMD by addressing different modes of action. JSM-6427 acts as an antagonist of the integrin α5β1 receptor. Integrin α5β1 is the prototype integrin and a therapeutic target in a final common pathway downstream of various blood vessel formation inducing factors including VEGF and bFGF (basic Fibroblast Growth Factor). JSM-6427 exhibits a 1700-fold selectivity for the α5β1 integrin and prevents α5β1 from binding to fibronectin, a glycoprotein that is an important component of the extracellular matrix that helps to maintain cell structure and function by acting (among others) as a binding site for cell surface receptors.
- 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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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
- 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
- General References
- Maier AK, Kociok N, Zahn G, Vossmeyer D, Stragies R, Muether PS, Joussen AM: Modulation of hypoxia-induced neovascularization by JSM6427, an integrin alpha5beta1 inhibiting molecule. Curr Eye Res. 2007 Sep;32(9):801-12. [Article]
- Umeda N, Kachi S, Akiyama H, Zahn G, Vossmeyer D, Stragies R, Campochiaro PA: Suppression and regression of choroidal neovascularization by systemic administration of an alpha5beta1 integrin antagonist. Mol Pharmacol. 2006 Jun;69(6):1820-8. Epub 2006 Mar 9. [Article]
- Zahn G, Vossmeyer D, Stragies R, Wills M, Wong CG, Loffler KU, Adamis AP, Knolle J: Preclinical evaluation of the novel small-molecule integrin alpha5beta1 inhibitor JSM6427 in monkey and rabbit models of choroidal neovascularization. Arch Ophthalmol. 2009 Oct;127(10):1329-35. doi: 10.1001/archophthalmol.2009.265. [Article]
- External Links
- Not Available
Clinical Trials
- Clinical Trials
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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
Drug created at November 18, 2007 18:30 / Updated at July 31, 2024 09:44