Abstract
RPR127963 demonstrates an excellent pharmacokinetic profile in several species and was found to be efficacious in the prevention of restenosis in a Yucatan mini-pig model upon oral administration of 1-5 mg/kg. The in vitro selectivity profile and SAR of the highly optimized PDGF-R tyrosine kinase inhibitor are highlighted.
MeSH terms
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Administration, Oral
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Animals
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Biological Availability
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Cell Division / drug effects
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Chemotaxis / drug effects
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Collagen / biosynthesis
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Cytochrome P-450 Enzyme System / biosynthesis
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / pharmacokinetics
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Enzyme Inhibitors / pharmacology
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Inhibitory Concentration 50
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Protein-Tyrosine Kinases / antagonists & inhibitors
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Quinoxalines / chemical synthesis*
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Quinoxalines / pharmacokinetics*
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Quinoxalines / pharmacology
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Rats
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Receptors, Platelet-Derived Growth Factor / antagonists & inhibitors*
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Structure-Activity Relationship
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Swine
Substances
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Enzyme Inhibitors
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Quinoxalines
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Collagen
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Cytochrome P-450 Enzyme System
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Protein-Tyrosine Kinases
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Receptors, Platelet-Derived Growth Factor