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Related Experiment Videos

Iloperidone (Hoechst Marion Roussel Inc).

J M Hesselink1

  • 1abfab@jmulder.demon.nl

Idrugs : the Investigational Drugs Journal
|August 30, 2005
PubMed
Summary

Iloperidone, an investigational drug for schizophrenia, targets serotonin 5-HT2 and dopamine D2 receptors. Despite initial discontinuation, Phase III trials are underway, focusing on its atypical antipsychotic potential and reduced side effects.

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Area of Science:

  • Pharmacology
  • Neuroscience
  • Clinical Trials

Background:

  • Iloperidone (HP-873) is a 5-HT2 antagonist investigated for schizophrenia and psychosis.
  • Development was initially discontinued by Hoechst Marion Roussel but later licensed to Titan Pharmaceuticals.
  • Novartis acquired global rights (excluding Japan) and initiated Phase III trials in 1998.

Purpose of the Study:

  • To evaluate the efficacy and safety of iloperidone in treating schizophrenia.
  • To assess the role of 5-HT2 and D2 receptor affinities in iloperidone's antipsychotic activity.
  • To determine the potential for reduced extrapyramidal side-effects compared to other antipsychotics.

Main Methods:

  • Phase III clinical trials involving 3000 patients across 20 countries.
  • Receptor binding assays to determine affinity for dopamine D2 and serotonin 5-HT2 receptors.
  • Pharmacological profiling of iloperidone's mechanism of action.

Main Results:

  • Iloperidone exhibits moderate affinity for D2 receptors and higher affinity for 5-HT2 receptors.
  • This receptor binding profile is associated with atypical antipsychotic activity.
  • The drug is being evaluated for its potential to minimize extrapyramidal side-effects.

Conclusions:

  • Iloperidone's dual receptor antagonism suggests potential as an atypical antipsychotic.
  • Ongoing Phase III trials are crucial for confirming its therapeutic value in schizophrenia.
  • The compound represents a significant development in the search for safer and more effective schizophrenia treatments.

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