Single Oral Dose Administration Of A Specific Thromboxane Synthetase Inhibitor To Normal Volunteers - A Double Blind Placebo Controlled Study

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Abstract
A specific thromboxane synthetase inhibitor (UK-37248-01) is a new imidazole derivative synthesised by Pfizer Central Research. In vitro and animal experiments showed the compound to be a potent, selective and orally active one. Six healthy male volunteers received a single dose of 100mg of a specific thromboxane synthetase inhibitor or a matching placebo in a double blind cross-over study, there being a 2 week interval between treatments. Production of thromboxane B2 in serum was markedly reduced 1 hour after the drug administration, with about 50% inhibition still evident at 6 hours. The drug had no effect no circulating β-thromboglobulin and platelet factor 4 antigen levels, or on platelet aggregation to ADP or collagen, though release of 5HT was reduced. Increase in bleeding time (2-3 minutes) was recorded in 3 volunteers 1 hour after the drug administration. Chemical assay of the compound showed that up to 45% of the oral dose was excreted in the urine within 24 hours; 90% of this was excreted within the first 4 hours. Routine haematology and clinical chemistry tests repeated 24 hours and 4 days after dosing gave no indication of drug related toxicity.

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