Objectives: Panomifene, PAN, /E/-1, 2-diphenyl-1-14-12-(2-hydroxyethy- amino)-ethoxyl-phenyl1-3, 3, 3-trifluoropropene is a new original Hungarian compound, structurally similar to tamoxifen, TMX. In the human phase l/a study the human tolerance, pharmacokinetics and endocrine effects of a single oral dose of PAN were evaluated in healthy, postmenopausal, female volunteers. The present paper describes the clinical pharmacokinetics of the drug. Methods: In the course of the dose escalation detailed pharmacokinetic studies were carried out at doses of 24, 48, 96 mg in two volunteers, 120 mg in one volunteer. At a selected dose level (24 mg) detailed pharmacokinetics were performed in 10 volunteers. Results: The pharmacokinetic study showed considerable interindividual variability of the parameters, the kinetics, however, was linear in the studied dose range. At the selected dose level (24 mg p. o.) the peak concentration of the plasma was 61,25±21,71 ng/ml, the time to peak was 3,33±1,68 hours. The mean of the terminal half-life was 71,97±23,64 hours, the area under the plasma concentration time curve (ALJC0-∞) 4007±1405 (nglml)x hours. Conclusions: According to the phase l/a study, the PAN seemed to be a safe TMX analogue, the single oral dose of which did not exert any noteworthy toxic side effect.
|Number of pages||4|
|Publication status||Published - Dec 1 1997|
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