PG-530742

Identification

Generic Name
PG-530742
DrugBank Accession Number
DB05495
Background

PG-530742 selectively inhibits certain matrix metalloproteinases that have been implicated in the cartilage degradation that occurs in osteoarthritis. By inhibiting these MMPs, it potentially limits cartilage degradation and disease progression. Studies are currently assessing the efficacy and safety of PG-530742 in the treatment of mild to moderate knee osteoarthritis.

Type
Small Molecule
Groups
Investigational
Synonyms
Not Available

Pharmacology

Indication

Investigated for use/treatment in osteoarthritis.

Pharmacology
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Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

PG-530742 selectively inhibits certain matrix metalloproteinases that have been implicated in the cartilage degradation that occurs in osteoarthritis. By inhibiting these MMPs, it potentially limits cartilage degradation and disease progression. Studies are currently assessing the efficacy and safety of PG-530742 in the treatment of mild to moderate knee osteoarthritis.

Mechanism of action

PG-530742 selectively inhibits certain matrix metalloproteinases: In an independent research study, the drug-treated group showed decreased levels of MMP-2, -3, -9, and -13.

TargetActionsOrganism
UMatrix metalloproteinase-9Not 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
Medicalerrors
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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
Not Available
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
F94T42GL80
CAS number
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

References

General References
  1. Morita H, Khanal S, Rastogi S, Suzuki G, Imai M, Todor A, Sharov VG, Goldstein S, O'Neill TP, Sabbah HN: Selective matrix metalloproteinase inhibition attenuates progression of left ventricular dysfunction and remodeling in dogs with chronic heart failure. Am J Physiol Heart Circ Physiol. 2006 Jun;290(6):H2522-7. Epub 2006 Jan 20. [PubMed:16428338]
PubChem Substance
347910172

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentHeart Enlargement / Heart Failure / Myocardial Infarction1
2CompletedTreatmentOsteoarthritis of the Knee1

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

Drugtargets
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Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
May play an essential role in local proteolysis of the extracellular matrix and in leukocyte migration. Could play a role in bone osteoclastic resorption. Cleaves KiSS1 at a Gly-|-Leu bond. Cleaves...
Gene Name
MMP9
Uniprot ID
P14780
Uniprot Name
Matrix metalloproteinase-9
Molecular Weight
78457.51 Da

Drug created on November 18, 2007 18:25 / Updated on June 12, 2020 16:52