M-100907 (Aventis).

Abstract

M-100907 is a highly selective 5-HT2A antagonist that is being developed by Aventis Pharmaceuticals, formerly Hoechst Marion Roussel (HMR), for the potential treatment of schizophrenia. M-100907 is in phase III trials for chronic schizophrenia [307936], [307942], [307940]. In August 1999, development was discontinued for acute schizophrenia (schizoaffective disorder) on the basis of poor results [335083]. M-100907 is a potent antagonist in every putative animal behavioral model of schizophrenia that involves activation of 5-HT2A receptors [181713]. Interestingly, M-100907 is also active in animal models involving blockade of NMDA glutamatergic channel receptors, an effect known to resemble some behavioral symptoms of schizophrenia in man [390328]. M-100907 belongs to a series of piperidine derivatives, which were originally disclosed in the associated patent, EP-00208235. M-100907 is specifically claimed in a later patent, EP-00531410. This patent describes superior in vivo potency for M-100907 and its claims include the use of M-100907 for the treatment of thromboembolic disorders. The use of M-100907 for the treatment of various developmental neurological disorders such as autism and attention deficit hyperactivity disorder is disclosed in WO-09956750. In 1996, this product was designated one of HMR's nine top priority products, serving an unmet medical need and addressing a potential market in excess of US $500 million per year [221118]. In January 1999, BT Alex Brown predicted sales of US $30 million in 2000 rising to US $220 million in 2002 [318220]. In April 1999, ABN Amro predicted annual sales of DM 50 million in 2000, rising to DM 150 million in 2002 [328676].

• Authors: T de Paulis
• Journal: Current opinion in investigational drugs (London, England : 2000) (Curr Opin Investig Drugs) Vol. 2 Issue 1 Pg. 123-32 (Jan 2001) ISSN: 1472-4472 [Print] England
• PMID: 11527004 (Publication Type: Journal Article)

Chemical References

• Fluorobenzenes
• Piperidines
• Receptor, Serotonin, 5-HT2A
• Receptors, Serotonin
• Serotonin Antagonists
• volinanserin

Topics

• Animals
• Clinical Trials as Topic
• Fluorobenzenes (pharmacology)
• Humans
• Piperidines (pharmacology)
• Receptor, Serotonin, 5-HT2A
• Receptors, Serotonin (drug effects)
• Serotonin Antagonists (chemical synthesis, pharmacology, therapeutic use)
• Structure-Activity Relationship