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Lesopitron (Esteve).

F Micheli1

  • 1GlaxoSmithKline, Medicines Research Centre, Chemistry Dept, Via Fleming 4, 37135 Verona, Italy. fm20244@glaxowellcome.co.uk

Idrugs : the Investigational Drugs Journal
|July 21, 2005
PubMed
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Lesopitron, a novel anxiolytic, demonstrates potent 5-HT1A agonist activity and good tolerability in early trials. It shows promise in treating anxiety disorders and withdrawal symptoms with low acute toxicity.

Area of Science:

  • Pharmacology
  • Neuroscience
  • Drug Development

Background:

  • Lesopitron is an anxiolytic agent developed by Esteve.
  • It exhibits pre- and post-synaptic 5-HT1A agonist activity.
  • The drug is currently in Phase II clinical trials in Spain and the US.

Purpose of the Study:

  • To evaluate the safety and efficacy of Lesopitron as an anxiolytic.
  • To investigate its pharmacological profile, including receptor interactions and effects in animal models of anxiety.
  • To assess its tolerability and potential long-term effects.

Main Methods:

  • Phase I trials in healthy volunteers to assess tolerability of single and repeated doses.
  • Preclinical studies using rat social interaction and marmoset anxiety models.

Related Experiment Videos

  • Evaluation of effects on alpha-adrenergic and dopaminergic receptors.
  • Assessment of acute toxicity and potentiation of alcohol/barbiturate effects.
  • Long-term usage studies to monitor metabolic parameters.

    • Main Results:

    • Lesopitron was well tolerated in single doses up to 50 mg and repeated doses up to 45 mg/day.
    • It demonstrated potent 5-HT1A agonist activity and was more effective than related compounds in animal models.
    • Negligible effects on alpha-adrenergic and dopaminergic receptors were observed.
    • The drug effectively countered benzodiazepine withdrawal-induced anxiety in rodents.
    • Low acute toxicity and no potentiation of alcohol or barbiturate effects were noted.
    • Long-term usage resulted in reductions in plasma glucose, triglycerides, phospholipids, and cholesterol.

    Conclusions:

    • Lesopitron is a well-tolerated anxiolytic with potent 5-HT1A agonist activity.
    • It shows efficacy in preclinical models of anxiety and withdrawal symptoms.
    • Further clinical trials are warranted to establish its therapeutic potential in humans.