Abstract
The discovery of a potent intracellular inhibitor of human neutrophil elastase which is orally active and has a long duration of action is described. The pharmacodynamic and pharmacokinetic properties of a trans-lactam development candidate, GW311616A, are described.
MeSH terms
-
Administration, Oral
-
Animals
-
Bacteria / drug effects
-
Bacterial Infections / drug therapy
-
Biological Availability
-
Cricetinae
-
Crystallization
-
Dogs
-
Drug Stability
-
Lactams / pharmacokinetics*
-
Lactams / pharmacology*
-
Leukocyte Elastase / antagonists & inhibitors
-
Leukocyte Elastase / metabolism
-
Metabolic Clearance Rate / physiology
-
Pancreatic Elastase / chemistry
-
Piperidines / chemistry*
-
Piperidines / pharmacokinetics
-
Piperidines / pharmacology*
-
Rats
-
Serine Endopeptidases / drug effects
-
Serine Endopeptidases / metabolism
-
Serpins / chemistry*
-
Serpins / pharmacokinetics
-
Serpins / pharmacology*
Substances
-
GW 311616
-
Lactams
-
Piperidines
-
Serpins
-
Serine Endopeptidases
-
Pancreatic Elastase
-
Leukocyte Elastase