NAV

REP8839

Identification

Generic Name
REP8839
DrugBank Accession Number
DB05224
Background

REP8839 is a novel methionyl-tRNA synthetase (MetS) inhibitor being developed by Replidyne (GlaxoSmithKline licensed REP8839 to Replidyne in June of 2003).

Type
Small Molecule
Groups
Investigational
Synonyms
Not Available
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Pharmacology

Indication

For the treatment of bacterial infections caused by susceptible microorganisms (Staphylococcus aureus, including methicillin-resistant S. aureus (MRSA), and Streptococcus pyogenes).

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Contraindications & Blackbox Warnings
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Pharmacodynamics

REP8839 is a novel methionyl-tRNA synthetase (MetS) inhibitor with potent antibacterial activity against clinical isolates of Staphylococcus aureus, Streptococcus pyogenes, and other clinically important gram-positive bacteria but little activity against gram-negative bacteria.

Mechanism of action

REP8839 exerts its antibacterial activity through specific inhibition of MetS, a novel target.

TargetActionsOrganism
UMethionine--tRNA ligaseNot AvailableStaphylococcus aureus (strain MRSA252)
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

REP8839 is highly bound to human serum proteins.

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

Not Available

Pathways
Not Available
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Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
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
  • Bacteria

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. Critchley IA, Young CL, Stone KC, Ochsner UA, Guiles J, Tarasow T, Janjic N: Antibacterial activity of REP8839, a new antibiotic for topical use. Antimicrob Agents Chemother. 2005 Oct;49(10):4247-52. [Article]
  2. Ochsner UA, Young CL, Stone KC, Dean FB, Janjic N, Critchley IA: Mode of action and biochemical characterization of REP8839, a novel inhibitor of methionyl-tRNA synthetase. Antimicrob Agents Chemother. 2005 Oct;49(10):4253-62. [Article]
PubChem Substance
347910034

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
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
Chromatographic Properties
Collision Cross Sections (CCS)
Not Available

Targets

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Details1. Methionine--tRNA ligase
Kind
Protein
Organism
Staphylococcus aureus (strain MRSA252)
Pharmacological action
Unknown
General Function
Trna binding
Specific Function
Is required not only for elongation of protein synthesis but also for the initiation of all mRNA translation through initiator tRNA(fMet) aminoacylation.
Gene Name
metG
Uniprot ID
Q6GJI1
Uniprot Name
Methionine--tRNA ligase
Molecular Weight
74896.93 Da
References
  1. Ochsner UA, Young CL, Stone KC, Dean FB, Janjic N, Critchley IA: Mode of action and biochemical characterization of REP8839, a novel inhibitor of methionyl-tRNA synthetase. Antimicrob Agents Chemother. 2005 Oct;49(10):4253-62. [Article]

Drug created at October 21, 2007 22:24 / Updated at June 12, 2020 16:52