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ESTEVE Announces the Publication of Comprehensive Phase I Data for a Novel Oral, First-in-class New Chemical Entity (NCE),E-52862, a Sigma-1 Receptor Antagonist (S1RA) Being Developed for Pain
Date:9/4/2012

works both independently and in collaboration to bring new, differentiated best-in-class treatments to patients who need them. The company currently has a team of about 2800 professionals, and has subsidiaries and production facilities in several European countries, USA, China and Mexico.

About E-52862 and Pain R&D at ESTEVE

ESTEVE's dedicated in-house R&D team is focused on the development of novel pain medications, an area of high unmet medical need. Considerable progress in the knowledge of the biology and pharmacology of the S1R (a unique protein) during recent years has re-energised research into the potential benefits of S1R ligands in a range of neurological and psychiatric conditions.

New data has addressed key questions on modulation, MOA and pathophysiology of the S1R. The proprietary knockout mouse demonstrated a direct role of the S1R in sensitisation phenomena associated with neuropathic pain mechanisms and behaviours.  E-52862 exerts robust, dose-dependent analgesic activity in multiple preclinical neuropathic pain models and enhances opioid analgesia. E-52862 could have potential applications for other neurological and psychiatric indications. Besides information reported here, an extensive preclinical regulatory safety package is available for E-52862 (including 13-week repeat dose toxicity studies in various animal species). E-52862 also has robust intellectual property protection.

ESTEVE's portfolio in pain also includes a technology platform-derived new co-crystal entity (E-58425) developed by the in-house R&D team. E-58425 has completed Phase I, with Phase II currently ongoing. E-58425 is being developed for moderate to severe acute and chronic pain.

Reference

[1]Abadias, M. et al.  Safety, Tolerability and Pharmacokinetics of Single and Multiple Doses of a Novel Sigma-1 Receptor Antagonist in Three Randomized Phase I Studies. Br J Clin Pharmaco
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