Explore a selection of our essential drug information below, or:
Overview
- DrugBank ID
- DB05468
- Type
- Small Molecule
- Clinical Trials
- Phase 0
- 0
- Phase 1
- 0
- Phase 2
- 0
- Phase 3
- 0
- Phase 4
- 0
Identification
- Generic Name
- R411
- DrugBank Accession Number
- DB05468
- Background
R411 is a non-steroid oral medicine for the treatment of asthma. It is not immunosuppressive, but blocks the activation and recruitment of cells involved in respiratory inflammation. It is a dual-acting competitive integrin antagonist (as compared to previously developed single integrin antagonists or SIAs) that prevents binding of V-CAM1 to either a4b1 or a4b7.
- Type
- Small Molecule
- Groups
- Investigational
- Synonyms
- Not Available
Pharmacology
- Indication
Investigated for use/treatment in asthma.
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R411 is a non-steroid oral medicine for the treatment of asthma. It is not immunosuppressive, but blocks the activation and recruitment of cells involved in respiratory inflammation. It is a dual-acting competitive integrin antagonist (as compared to previously developed single integrin antagonists or SIAs) that prevents binding of V-CAM1 to either a4b1 or a4b7.
- Mechanism of action
R411 prevents binding of V-CAM1 to either a4b1 or a4b7.
Target Actions Organism UIntegrin alpha-4 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
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Good safety profile observed in preclinical and clinical studies
- 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
- Hijazi Y, Welker H, Dorr AE, Frank K, Renzetti LM, Patel I: Evaluation of the effect of multiple-dose administration of R411, a dual alpha4beta1-alpha4beta7 integrin antagonist on the major CYP isoform activities in healthy volunteers. Eur J Clin Pharmacol. 2006 Jan;62(1):83-5. Epub 2005 Dec 21. [Article]
- Hijazi Y, Welker H, Dorr AE, Tang JP, Blain R, Renzetti LM, Abbas R: Pharmacokinetics, safety, and tolerability of R411, a dual alpha4beta1-alpha4beta7 integrin antagonist after oral administration at single and multiple once-daily ascending doses in healthy volunteers. J Clin Pharmacol. 2004 Dec;44(12):1368-78. [Article]
- External Links
- PubChem Substance
- 347910156
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
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Integrins alpha-4/beta-1 (VLA-4) and alpha-4/beta-7 are receptors for fibronectin. They recognize one or more domains within the alternatively spliced CS-1 and CS-5 regions of fibronectin. They are also receptors for VCAM1. Integrin alpha-4/beta-1 recognizes the sequence Q-I-D-S in VCAM1. Integrin alpha-4/beta-7 is also a receptor for MADCAM1. It recognizes the sequence L-D-T in MADCAM1. On activated endothelial cells integrin VLA-4 triggers homotypic aggregation for most VLA-4-positive leukocyte cell lines. It may also participate in cytolytic T-cell interactions with target cells. ITGA4:ITGB1 binds to fractalkine (CX3CL1) and may act as its coreceptor in CX3CR1-dependent fractalkine signaling (PubMed:23125415). ITGA4:ITGB1 binds to PLA2G2A via a site (site 2) which is distinct from the classical ligand-binding site (site 1) and this induces integrin conformational changes and enhanced ligand binding to site 1 (PubMed:18635536, PubMed:25398877). Integrin ITGA4:ITGB1 represses PRKCA-mediated L-type voltage-gated channel Ca(2+) influx and ROCK-mediated calcium sensitivity in vascular smooth muscle cells via its interaction with SVEP1, thereby inhibiting vasocontraction (PubMed:35802072)
- Specific Function
- cell adhesion molecule binding
- Gene Name
- ITGA4
- Uniprot ID
- P13612
- Uniprot Name
- Integrin alpha-4
- Molecular Weight
- 114898.745 Da
Drug created at November 18, 2007 18:25 / Updated at June 12, 2020 16:52