Tolerability and pharmacokinetics of ebrotidine in healthy subjects given single and repeated oral doses

Magí Farré, Pere N. Roset, Josep M. Badenas, Balbina Ugena, Miguel Márquez, Carlos Albet, Eduardo Herrero, José A. Ortiz

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4 Citations (Scopus)


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.
Original languageEnglish
Pages (from-to)528-530
JournalArzneimittel-Forschung/Drug Research
Issue number4 A SPEC. ISSUE
Publication statusPublished - 24 Jun 1997


  • CAS 100981-43-9
  • Ebrotidine
  • FI-3542, clinical pharmacokinetics, phase I study, tolerability
  • H -Receptor antagonist 2


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