New butyrophenones have been shown to treat psychosis in vivo but unlike the standard drug haloperidol, does not produce Parkinsonism-like movement disorders. On the other hand, these compounds are as potent as clozapine but do not interact with receptors associated with the induction of weight gain.
Background:
Psychosis and specifically schizophrenia, is a very debilitating illness that has devastated the lives of many and their families. In the US, 1.1% of the population or about 4.1 million have been diagnosed with schizophrenia. Out of this number, up to a third of patients are treatment-resistant (TRS) and do not benefit from the medications currently available. In addition, schizophrenia is associated with suicidal ideation and somewhere between 9-13% of patients eventually take their own lives. Even more troubling is the fact that 65 to 80 % of outpatients with chronic schizophrenia discontinue their antipsychotic medications, often because of a lack of efficacy or intolerable adverse effects. Thus, new medications are urgently needed to replace those in current use.
Statement of Problem:
Of the two types of drugs currently used in the treatment of schizophrenia, the typical antipsychotics are very effective in treating the positive symptoms such as hallucinations, but they also produce serious movement disorders that often result in patients discontinuing the medications. Although still used, they have now been largely replaced by the atypical antipsychotics such as olanzapine. While movement disorders are generally lower with atypical antipsychotics, they often induce weight gain, metabolic disorders and Type II diabetes. Thus, new antipsychotic medications must overcome not only movement disorders but must not induce weight gain.
Potential Solution:
Based on the knowledge of the receptors responsible for the serious side effects, we have designed and now obtained new compounds demonstrated in animal studies to be as effective as clozapine but without neither the movement disorders or the weight gain even when tested at 5 times the therapeutic dose. Indeed, in a head to head evaluation of the binding profiles of the new agents with atypical antipsychotic agents currently in the clinic, the therapeutic potentials were superior in several cases. These compounds can be obtained in just three steps.
The Benefits:
New drugs will treat schizophrenia without producing movement disorders.
Drugs do not demonstrate the potential to produce weight gain or Type II diabetes,
Drug administration is similar to that employed in connection with olanzapine.
Commercialization Status:
Haloperidol analogs are currently in the pre-clinical development stage, and R&D is currently funded by the National Institutes of Health, NIGMS/MBRS Program. Validation of the observed activities in larger animal models is planned along with additional pharmacokinetic studies. We seek venture capitalists and partners or licensees with small molecule interest developments in the Biotechnology and/or Pharmaceutical Industries for commercialization.
Key Features:
Potential replacements for current antipsychotics without the associated weight gain or movement disorders.
Technology:
Drug replacements for the treatment of psychosis
Commercialization Status:
Haloperidol analogs are currently in the pre-clinical development stage, and R&D is currently funded by the National Institutes of Health, NIGMS/MBRS Program. Validation of the observed activities in larger animal models is planned along with additional pharmacokinetic studies. We seek venture capitalists and partners or licensees with small molecule interest developments in the Biotechnology and/or Pharmaceutical Industries for commercialization.
