Identification

Name
R667
Accession Number
DB05467
Description

R667 is an orally active, gamma selective retinoid agonist that shows promise as a treatment for emhysema, as it has, in animal models, promoted structural lung repair and functional improvement with fewer side effects. It is currently in Phase II Trials for emphysema secondary to alpha-1 antitrypsin deficiency.

Type
Small Molecule
Groups
Investigational
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Synonyms
Not Available

Pharmacology

Indication

Investigated for use/treatment in emphysema.

Contraindications & Blackbox Warnings
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Pharmacodynamics

R667 is an orally active, gamma selective retinoid agonist that shows promise as a treatment for emhysema.

Mechanism of action

Gamma-selective retinoic acid receptor agonist.

TargetActionsOrganism
URetinoic acid receptor gammaNot AvailableHumans
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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Toxicity

Well tolerated in patients with emphysema. no safety concerns have been identified.

Affected organisms
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

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
  1. Chiu YY, Roth MD, Kolis S, Rogovitz D, Davies B: Pharmacokinetics of a novel agent, R667, in patients with emphysema. Br J Clin Pharmacol. 2007 May;63(5):527-33. Epub 2007 Feb 23. [PubMed:17324249]
  2. Brennan BJ, Brown AB, Kolis SJ, Rutman O, Gooden C, Davies BE: Effect of R667, a novel emphysema agent, on the pharmacokinetics of midazolam in healthy men. J Clin Pharmacol. 2006 Feb;46(2):222-8. [PubMed:16432274]
  3. Brennan B, Chiu Y, Berthelon L, Kolis S, Davies B: Effect of age and gender on the pharmacokinetics of R667, a novel agent for the treatment of emphysema, in healthy volunteers. J Pharm Pharm Sci. 2007;10(1):9-16. [PubMed:17498389]
PubChem Substance
347910155

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

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

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expressi...
Gene Name
RARG
Uniprot ID
P13631
Uniprot Name
Retinoic acid receptor gamma
Molecular Weight
50341.405 Da
References
  1. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235]

Drug created on November 18, 2007 11:25 / Updated on June 12, 2020 10:52

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