Title : Clinical pharmacology of lumiracoxib: a selective cyclo-oxygenase-2 inhibitor.

Pub. Date : 2005

PMID : 16372823






5 Functional Relationships(s)
Download
Sentence
Compound Name
Protein Name
Organism
1 Lumiracoxib possesses a carboxylic acid group that makes it weakly acidic (acid dissociation constant [pKa] 4.7), distinguishing it from other selective COX-2 inhibitors. lumiracoxib mitochondrially encoded cytochrome c oxidase II Homo sapiens
2 These data suggest that lumiracoxib may be associated with reduced systemic exposure, while still reaching sites where COX-2 inhibition is required for pain relief. lumiracoxib mitochondrially encoded cytochrome c oxidase II Homo sapiens
3 Major metabolites of lumiracoxib in plasma are the 5-carboxy, 4"-hydroxy and 4"-hydroxy-5-carboxy derivatives, of which only the 4"-hydroxy derivative is active and COX-2 selective. lumiracoxib mitochondrially encoded cytochrome c oxidase II Homo sapiens
4 Lumiracoxib is selective for COX-2 compared with COX-1 in the human whole blood assay with a ratio of 515 : 1 in healthy subjects and in patients with osteoarthritis or rheumatoid arthritis. lumiracoxib mitochondrially encoded cytochrome c oxidase II Homo sapiens
5 COX-2 selectivity of lumiracoxib is associated with a reduced incidence of gastroduodenal erosions compared with naproxen and a lack of effect on both small and large bowel permeability. lumiracoxib mitochondrially encoded cytochrome c oxidase II Homo sapiens