The tolerability and safety of ebrotidine (N-[(E)-[[2-[[[2- [(diaminomethylene)amino]-4-thiazolyl]methyl]thio]ethyl]amino] methylene]-4- bromo-benzenesulfonamide, CAS 100981-43-9, FI-3542) and its basic pharmacokinetic parameters were determined after its oral administration to healthy volunteers. Sixteen subjects were selected to participate in two different studies: an increasing single dose study to determine the maximal tolerated dose (from 25 to 1600 mg), and a multiple dose study (stepped doses from 400 to 1600 mg daily for 12 days). The results of the studies showed that ebrotidine has a good tolerability. Vital signs and laboratory tests were not influenced by the study treatment. No clinically relevant adverse effects were reported during the investigation. Ebrotidine reached peak plasma concentrations 2-3 h after oral administration. Its elimination half- life ranged from 9 to 14 h. In conclusion, ebrotidine was well tolerated after administration of oral single doses of up to 1600 mg, and after repeated administration of up to 800 mg/12 h for 12 days.
|Issue number||4 A SPEC. ISSUE|
|Publication status||Published - 24 Jun 1997|
- CAS 100981-43-9
- FI-3542, clinical pharmacokinetics, phase I study, tolerability
- H -Receptor antagonist 2