Dopamine D2 receptor occupancy (D2RO) is a key feature of all currently approved antipsychotic medications. However, antipsychotic efficacy associated with high D2RO is often limited by side effects such as motor disturbances and hyperprolactinemia. Lumateperone (ITI-007) is a first-in-class selective and simultaneous modulator of serotonin, dopamine and glutamate in development for the treatment of schizophrenia and other disorders. The primary objective of the present study was to determine D2RO at plasma steady state of 60 mg ITI-007, a dose that previously demonstrated antipsychotic efficacy in a controlled trial, administered orally open-label once daily in the morning for two weeks in patients with schizophrenia (N = 10) and after at least a two-week washout period from standard of care antipsychotics. D2RO was determined using positron emission tomography with 11C-raclopride as the radiotracer. Mean peak dorsal striatal D2RO was 39% at 60 mg ITI-007 occurring 1 h post-dose. Lumateperone was well-tolerated with a favorable safety profile in this study. There were no clinically significant changes in vital signs, ECGs, or clinical chemistry laboratory values, including prolactin levels. There were no adverse event reports of akathisia or other extrapyramidal motor side effects; mean scores on motor function scales indicated no motor disturbances with lumateperone treatment. This level of occupancy is lower than most other antipsychotic drugs at their efficacious doses and likely contributes to the favorable safety and tolerability profile of lumateperone with reduced risk for movement disorders and hyperprolactinemia. If approved, lumateperone may provide a new and safe treatment option for individuals living with schizophrenia.
Anyone wanna save me some time and tell me the point reduction of symptoms with this drug?
I think the average was 14 points.
is this the newest drug?
It’s not out yet, it is in the approval process.
It seems likely that it will be approved and available in 2019.
R2d2 drug 151515155
how is it bettter do you know?
Regardless the anti-psychotic efficacy ,there are two important statements in this report.
1- “If approved,lumateperone may provide a new and safe treatment OPTION for individuals living with schizophrenia”
2- " administered orally open-label once daily in the Morning for Two Weeks…and after at least a Two-week washout period "
Treatment OPTION,it means,the designer of anti-psychotic drug knows that,the drug is not a determined medication for a particular genetic disease
In all genetic disease,the medication is determined and there is no individual option (take it or not)
The drug is just a treats for a particular chemical symptom in the cell protein (D2)
and this means that,the cause who is responsible to developing a change in the protein (D2)
is not rooted from the basic genetic functions of the gene
In the case,if the change in the protein (D2) is a result of genetic disease,the medication treatment by anti-psychotic drug must be for lifetime -and there is no OPTION
I.E the change in the D2 is not a symptom of inherited genetic disease
What is evidence ?
Look at this statement " administered…for two weeks "!
To avoid the side effects of anti-psychotic drug on the biochemistry of the brain,the treatment period must be between 2-weeks to 4-weeks -not for lifetime like all genetic diseases
This period of time is parallel the time of treatment the secondary symptoms of the viral disease-like flu ,whereas the patient can not using antibiotic for lifetime !
It must be there are objectivity causes to understand/explain this correspondence
Whether it’s better for you is probably a question for your doctor, but it’s supposed to modulate dopamine, serotonin, and glutamate, and it has a much lower dopamine occupancy. So it shouldn’t have the problems of TD. It’s also not supposed to result in blood sugar increases, heart issues, or weight gain.
My guess is that this is the first of a new generation of APs. 3rd generation, if you like. Although officially I don’t know if they are calling this a 2nd generation AP or not.
It is important to study the effect of sz cause on both of the mental side and chemical background from the Sz emanation moment for the next 24-48 hours,because it is a fateful moments in sz history
After the sz birth moment,there is no self biological defenses or psychological to blocking the sz pathway
All personal behavioral attempts that be done by the individual to resistance the sz effect will increase the impairment features ,nothing can stop the sz path towards the collapse
Regardless the bad effect of the cognitive changes,emotional,behavioral and chemical,the continuance of biological life itself in these conditions has becomes in dangerous state ( loss the chemical energy without cutout/ loss the ability to sleep /loss the rest state ).
the person in a state of waking up all time of day by day without sleeping or rest
the main task of the medical intervention is a way to safe the biological life itself,not a way to treatment specific disease or symptom
The sleep mechanism is the only natural way to blocking the sz pathway completely ,but it is not applicable by the self biological functions or self will ,therefor the medical intervention is necessary action (obligated) to blocking the sz pathways (temporarily)
Creation a chemical conditions by chemical drug in order to activates the sleep mechanism forcibly (the continuance of waking state all time of the day has becomes a wasteful factor for the chemical energy )
But to activate the rest state by chemical drug while the person in waking up do not cutoff both of cognitive changes and chemical imbalance features
After the first dose of medical treatment ,and having the ability to sleep in the existence of sz cause effects,is the fit indicator to protecting the biological life continuance
For about 2 -4 weeks ,the medical intervention is necessary (obligated),but after 4 weeks the medical treatment is optional for limited time to avoid the bad side effects of drugs on the biochemistry of brain ,because there is no actual organic disease substance in the anatomical structure
The important questions;
What are the preceding processes that has been occurred in brain cells and causing the changes that has been intervened on the quantity,speed and repetition rates of dopamine,serotonin ,and glutamate ?
what is the root origin of the chemical change ?
(What is the thing that coding (driving) the chemical change ?)
Most people imagine that,there is a defective gene,a negative mutation in the basic structure of gene (S),an anatomical changes in some areas of the brain , functional imperfection of proteins,a fault in the immune system…etc the self biological factors
But the final outcomes of the medical treatment do not agree with the theoretical image
We are in full overconfidence know that,there is external factor (not a natural part from the genetic material or/ the psychiatric component or the environmental factors) who is the driver of the chemical changes)
The internal logic of the chemical changes not related the self genetic functions,and over all rational expectations ,because the driver has coding/decoding a cognitive processes directly in the conscious state outside the genetic system or psychological self will ,the feedback of these processes in turn will coding the chemical changes in the cell proteins
According to the number of the cognitive processes in the time unties >>the quantity,the speed ,the repetition rate and direction will be determined chemically
Emission of the spoken thought in the conscious state will coding the chemical change
Each single spoken thought be broadcasting in the conscious mind/brain is just a pronounced code which translated into chemical equivalent
I know,it is hard to imagine an external factor has the functional capacity to driving the chemical change ,has the full ability to creates the thought inside the time-place of the conscious mind/brain forcibly (like a thought injection process),add for that the external factor have not a mass,external body ,cell structure,wall or nucleus and can not practices any biological functions at all ,and quintessential in coding/decoding all higher cognitive processes
Weather,if you understanding the truth or misunderstanding,believe or not believe,you should aware that the medical treatment can not make any direct effect on the external factor along sz lifetime,because it has not an organic structure,chemical substance and it is not working in the human chemical background directly,this external factor has working only in the conscious state as a center of continual disorder for lifetime
Therefore,all current medical treatment has an direct effect on the biochemistry of the brain ,in the same time there is no any direct effect on the external factor ,and external factor will sties alive/existent all lifetime in the human nature----- you must avoid development a bad side effect of the drugs in the long-term usage !
@panoramic20 what kind of medication you take now? You seem manic to me and i can’t read your posts.