M-100907 (Aventis).
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].
de Paulis
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Psychiatry Department, Vanderbilt University School of Medicine, Nashville, TN 37232, USA. Tomas.dePaulis@mcmail.vanderbilt.edu
D000818:Animals; D002986:Clinical Trials as Topic; D005464:Fluorobenzenes / Q000494:pharmacology*; D006801:Humans; D010880:Piperidines / Q000494:pharmacology*; D044402:Receptor, Serotonin, 5-HT2A; D011985:Receptors, Serotonin / Q000187:drug effects*; D012702:Serotonin Antagonists / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D013329:Structure-Activity Relationship
D005464:Fluorobenzenes; D010880:Piperidines; D044402:Receptor, Serotonin, 5-HT2A; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; C079049:volinanserin