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Abstract
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 B2 of ≤ 40% in association with an increase in prostaglandin E2. 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.
Disclosure
L Howes has previously acted as a consultant for Novogen Ltd, and is in receipt of payment for the conduct of Phase I clinical trials as well as other trials from Novogen. MJ James is in receipt of payment for the conduct of preclinical work on NV-52. T Florin is a member of the advisory board to Novogen and is a consultant for the company. C Walker is a full-time employee of Novogen.