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ESTEVE Announces Publication of Key Preclinical Data for a Novel Oral, First-in-class New Chemical Entity (NCE) Sigma-1 Receptor Antagonist (E-52862), that has Completed Phase I and Initiated its Phase II Clinical Trial Program
Date:7/17/2012

BARCELONA, July 17, 2012 /PRNewswire/ --

  • The sigma-1 receptor (S1R) is an important development target for innovative medications to treat neuropathic pain, for which new medications are much needed.
  • Developed by ESTEVE, E-52862 is a potent, highly selective NCE with a novel mechanism of action (S1R antagonism) currently being evaluated for the treatment of pain.
  • In studies conducted to date in preclinical models, a direct relationship between dose of E-52862, levels of E-52862 interacting with the S1R in the brain, and analgesic activity (pain-relieving effect) was demonstrated.
  • Importantly, in these models, the pain-relieving effect of E-52862 is maintained with repeated treatment.
  • E-52862 has completed a rigorous Phase I programme that included more than 300 subjects.  Results show good safety, tolerability, pharmacodynamic and pharmacokinetic profiles.
  • Phase II clinical trials evaluating E-52862 are ongoing.

ESTEVE announces the recent publication in the British Journal of Pharmacology[1] of important preclinical data that furthers understanding of its highly potent and selective, once-daily, S1R antagonist E-52862, developed by the ESTEVE Research and Development (R&D) team.

José Miguel Vela, PhD, responsible for ESTEVE Drug Discovery and Preclinical Development, stated, "These data demonstrate the role of ESTEVE's E-52862, a NCE from our programme of sigma-1 receptor antagonists, as a novel modulator of pain sensitisation and relief.  It also highlights that the target of this new compound, the sigma-1 receptor, is correlated mechanistically with the compound's ability to relieve pain."

Key data reported in the publication highlight the pharmacological activity of the selective S1R antagonist E-52862, which acts on the central nervous system (CNS) in various preclinical models of pain.  
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