Intra-Cellular Therapies, Inc., 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.
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.
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