Navigation Links
Intra-Cellular Therapies Announces the Discovery of Potent Antidepressant Activity in ITI-007

NEW YORK, April 9, 2008 /PRNewswire/ -- Intra-Cellular Therapies, Inc., today announced additional preclinical data from its ongoing development programs for ITI-007, the Company's first-in-class dual 5HT2A receptor antagonist/dopamine receptor phosphoprotein modulator (DPPM), and ITI-722, a low-dose formulation of ITI-007, which are in development for schizophrenia and sleep disorders, respectively. These new data demonstrate ITI-007 has preclinical activity both in vitro and in vivo as an antidepressant.

ITI-007 acts as a potent inhibitor of the serotonin transporter (SERT), a major target for most antidepressant drugs. To examine whether this in vitro activity could be predictive of behavioral activity in vivo, the antidepressant effect of ITI-007 was investigated using an animal model of depression involving social stress. Repeated treatment of ITI-007 improved performance in this animal model, consistent with antidepressant-like efficacy. The combined actions of ITI-007 as a SERT inhibitor, a 5HT2A receptor antagonist, and a DPPM may provide a unique, antidepressant drug with a more optimal profile, including a lack of sexual side effects common to other antidepressant drugs.

"These studies demonstrate ITI-007 may have antidepressant activity in addition to its potential in treating sleep maintenance insomnia and psychosis in patients," stated Sharon Mates, Ph.D., Chairman and Chief Executive Officer of Intra-Cellular Therapies. "We believe ITI-007 represents a unique compound that may have broad use in treating many neuropsychiatric and neurodegenerative disorders where sleep problems, depression, or psychosis are prominent symptoms, including schizophrenia, affective disorders, and Parkinson's disease."

About ITI-007

ITI-007 is an orally available compound which combines potent 5HT2A receptor antagonism with cell-type-specific modulation of phosphoprotein pathways downstream of dopamine receptors. As a dopamine receptor phosphoprotein modulator (DPPM), ITI-007 has dual properties; it acts as a post-synaptic antagonist and as a pre-synaptic partial agonist. The combination of ITI-007's high-potency blockade of 5HT2A receptors and unique dopamine receptor activity will make it possible for the first time, to select a clinical dose capable of saturating 5HT2A receptors while permitting the "dialing in" of an optimal amount of dopamine receptor modulation. The ability to optimize the level of dopamine receptor modulation holds promise for the reduction of psychotic symptoms without incurring high levels of dopamine antagonism that cause motor disturbances and other deleterious side effects. In addition, the wide separation of affinity at 5HT2A and D2 receptors may allow for administration of the appropriate amount of dopamine modulation for antipsychotic maintenance therapy in the treatment of bipolar disorders. ITI-007 also has nanomolar affinity for the serotonin transporter (SERT). ITI-007 has a much lower propensity than several currently marketed antipsychotic drugs to bind receptors that mediate deleterious cardiovascular events, sedation and rapid and significant weight gain.

About ITI-722

A low-dose formulation of ITI-007, called ITI-722, is being developed simultaneously for the treatment of sleep maintenance insomnia in the general population. Due to the unique separation of D2 and 5HT2A receptor affinities, at low doses, ITI-722 acts primarily as a 5HT2A receptor antagonist. Additionally, its profile suggests the compound may be appropriate for the treatment of sleep disorders that accompany neurodegenerative disorders, such as Parkinson's disease.

About Depression

Depression is a common psychiatric disorder affecting approximately 20 million people in the United States. It is characterized by a pervasive low mood, loss of interest in usual activities and diminished ability to experience pleasure. Although the term "depression" is commonly used to describe a temporarily depressed mood when one "feels blue," clinical depression is a serious and often disabling condition that can significantly affect a person's work, family and school life, sleeping and eating habits, general health, and ability to enjoy life. Having depression is also a major risk factor for suicide; in addition, people with depression suffer from higher mortality from other causes. Moreover, depression is a common co- morbid diagnosis in schizophrenia, being present in over 30% of people with schizophrenia in many studies.

About Intra-Cellular Therapies

Intra-Cellular Therapies, Inc. (ITI), is a biopharmaceutical company that is developing novel drugs for the treatment of diseases and disorders of the Central Nervous System (CNS). Building on the science generated from the Nobel Prize winning laboratory of Dr. Paul Greengard at The Rockefeller University, the Company develops compounds that have the potential to treat a wide range of diseases associated with the CNS. To aid in the development process, the Company incorporates its CNSProfile(TM), a state-of-the-art platform that allows ITI to choose compounds with the strongest potential to succeed in these difficult to treat diseases.

SOURCE Intra-Cellular Therapies, Inc.
Copyright©2008 PR Newswire.
All rights reserved

Related medicine technology :

1. Intra-Cellular Therapies Presents Preclinical Data From Schizophrenia and Sleep Maintenance Programs
2. Intra-Cellular Therapies Initiates Phase 2 Clinical Trial for Sleep Maintenance Insomnia
3. Intra-Cellular Therapies Presents Data on Its Schizophrenia and Cognition in Schizophrenia Programs at the 14th Biennial Winter Workshop on Schizophrenia and Bipolar Disorders
4. Intra-Cellular Therapies Announces the Discovery of Potent Antidepressant Activity in ITI-007/ITI-722
5. LigoCyte Pharmaceuticals Announces Collaboration With Biogen Idec to Develop Anti-CD103 Therapies
6. ActiveSight and CHDI Leverage Fragment-Based Lead Discovery for Huntington Disease Therapies
7. New Data Show Doripenem as Effective as Commonly Used Therapies in Treating Hospital-Acquired Pneumonias
8. NIST Awards $2 Million to Velcura Therapeutics, Inc. for Innovative Technology R&D - Dual-Action Therapies for Bone Disease
9. Studies Attribute Recent Increase in Multiple Myeloma Survival to Novel Therapies
10. Vital Therapies Announces Presentation of ELAD(R) Artificial Liver Data at American Association for the Study of Liver Diseases 2007 Annual Meeting
11. New Data to Support VELCADE(R) (Bortezomib) For Injection Based Therapies as Setting New Standards in The Care of Newly Diagnosed Patients With Multiple Myeloma
Post Your Comments:
(Date:11/30/2015)... Asia,s largest exhibition and conference dedicated to the Medical Device ... 22 nd April 2016. --> --> ... --> -->   --> --> ... population and the government back up, the Medical Device is one of the ... . With the aging population and the government back up, the Medical ...
(Date:11/30/2015)... REDWOOD CITY, Calif. , Nov. 30, 2015 ... company that is providing innovative evidence-based solutions for the treatment ... Appeals Board (PTAB) at the U.S. Patent and Trademark Office ... (IPR) of U.S. Patent No. 8,359,102 (the ,102 patent).  ... 14, 2015, a unit of Boston Scientific Corporation filed two ...
(Date:11/30/2015)... ) has ... Market 2015-2019" report to their offering. ... of the "Orphan Drugs Market 2015-2019" ... and Markets ( ) has announced the ... report to their offering. ...
Breaking Medicine Technology:
(Date:11/30/2015)... ... 30, 2015 , ... Trevor and Taylor Crabb have unveiled an exciting new ... to represent the United States. This hybrid crowdfunding campaign is designed to ... journey in addition to offering corporate sponsors with some great marketing deliverables with the ...
(Date:11/30/2015)... ... 2015 , ... The National Association of Professional Women (NAPW) honors ... Year Circle. She is recognized with this prestigious distinction for leadership in estate sales ... more than 850,000 members and over 200 operating Local Chapters. , “I’m pleased to ...
(Date:11/30/2015)... ... December 01, 2015 , ... Live Very Well is ... insurance plans on . The multi-carrier insurance exchange platform offers individual ... allowing consumers to compare, quote and match plans to meet their needs. ...
(Date:11/30/2015)... (PRWEB) , ... November 30, 2015 , ... ... Foundation (Meso Foundation) released information for caregivers and held two webinars on topics ... available on demand free of charge at . , With a ...
(Date:11/30/2015)... ... November 30, 2015 , ... ... is proud to announce that its ThermiRFR temperature controlled radiofrequency platform has received ... innovative multi-application radiofrequency platform which uses temperature as a clinical endpoint. The ...
Breaking Medicine News(10 mins):