Nv-52: a novel thromboxane synthase inhibitor for the treatment of inflammatory bowel disease.
NV-52, a synthetic flavonoid derivative, is a selective thromboxane synthase (TXS) inhibitor that is being developed as a treatment for inflammatory bowel disease. NV-52 selectively inhibits TXS in vitro in physiological relevant concentrations, causing a reduction in thromboxane B(2) of </= 40% in association with an increase in prostaglandin E(2). NV-52 is effective in suppressing colonic inflammation in a murine model of inflammatory bowel disease. NV-52 has not demonstrated any toxicity in in vitro and animal toxicological studies, and has been administered to normal volunteers in a Phase I clinical trial without detectable adverse effects. NV-52 is well absorbed and a single dose of 400 mg p.o. produced a plasma concentration that is comparable with the concentrations that have been shown to produce significant TXS inhibition in vitro.
Howes
Laurence Guy
LG
Griffith and Bond University Medical Schools, Gold Coast Hospital, Southport, Queensland, Australia. laurie_howes@health.qld.gov.au
James
Michael John
MJ
Florin
Timothy
T
Walker
Catherine
C
D000818:Animals; D015507:Drugs, Investigational / Q000494:pharmacology / Q000627:therapeutic use; D004791:Enzyme Inhibitors / Q000494:pharmacology / Q000627:therapeutic use*; D005419:Flavonoids / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D015212:Inflammatory Bowel Diseases / Q000188:drug therapy* / Q000201:enzymology*; D013930:Thromboxane-A Synthase / Q000037:antagonists & inhibitors* / Q000378:metabolism
D015507:Drugs, Investigational; D004791:Enzyme Inhibitors; D005419:Flavonoids; C523002:Nv 52 compound; D013930:Thromboxane-A Synthase