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(12) Patent Application Publication (10) Pub. No.: US 2010/0113483 A1 SINGH (43) Pub US 20100113483A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2010/0113483 A1 SINGH (43) Pub. Date: May 6, 2010 (54) COMPOSITIONS OF 5-HT3 ANTAGONISTS (60) Provisional application No. 60/817,666, filed on Jun. AND DOPAMINE D2 ANTAGONSTS FOR 29, 2006. TREATMENT OF DOPAMNE-ASSOCATED CHRONIC CONDITIONS Publication Classification (51) Int. Cl. (76) Inventor: NIKHILESH N. SINGH, Mill A 6LX 3/59 (2006.01) Valley, CA (US) A6IP 25/30 (2006.01) Correspondence Address: (52) U.S. Cl. ................................................... S14/259.41 O'Melveny & Myers LLP (57) ABSTRACT IP&T Calendar Department LA-13-A7 400 South Hope Street The present invention provides novel compositions compris Los Angeles, CA 90071-2899 (US) ing a combination of a 5-HT receptor antagonist and a selec tive dopamine D receptor antagonist for the treatment of (21) Appl. No.: 12/684,024 obsessive, impulsive and compulsive behavioral activities and other dopamine pathway-associated disorders or condi tions. Preferably, the pharmaceutical compositions of the (22) Filed: Jan. 7, 2010 present invention comprise amounts of the 5-HT receptor antagonist ondansetron and a selective dopamine D receptor Related U.S. Application Data antagonist, Such as risperidone or olanzapine, that are suffi (63) Continuation of application No. 1 1/780.442, filed on cient to control a Subject's obsessive, impulsive and compul Jul.19, 2007, now abandoned, which is a continuation sive behavioral activities. Kits comprising the combination of of application No. 1 1/824,201, filed on Jun. 28, 2007, antagonists for the treatment of addictive disorders such as now abandoned. alcohol dependence are also provided. US 2010/0113483 A1 May 6, 2010 COMPOSITIONS OF 5-HT3 ANTAGONSTS the dopamine D receptor site. Alcohol or any alcohol-related AND DOPAMINE D2 ANTAGONSTS FOR cue Stimulates the release of dopamine through activation of TREATMENT OF DOPAMINE-ASSOCATED the 5-HT receptors on mesolimbic dopamine neurons, which CHRONIC CONDITIONS culminates in an interaction between free dopamine and the dopamine D receptor on the neuron. The role of dopamine on RELATED APPLICATIONS craving and the effects of alcohol on craving are Supported by studies involving dopamine Dantagonists such as haloperi 0001. This application is a continuation of U.S. applica dol and tiapride. Haloperidol was reported to block increases tion Ser. No. 11/780,442, filed Jul. 19, 2007, which is a in craving after priming doses of alcohol and tiapride effec continuation of U.S. application Ser. No. 1 1/824,201, filed tively increased abstinence among alcoholics. These clinical Jun. 28, 2007, which claims the benefit of U.S. Provisional findings with haloperidol and tiapride, however, are tempered Application Ser. No. 60/817,666, entitled “Compositions and due to extrapyramidal side-effects caused by simultaneous D. Methods for Treating Alcohol Dependence filed Jun. 29. antagonist activity of the drugs. 2006, all of which are hereby expressly incorporated by ref 0007 Three drugs are currently approved in the U.S. for erence in their entirety. the treatment of alcohol dependence: disulfiram; naltrexone: and acamprosate. Disulfiram, an aldehyde dehydrogenase BACKGROUND OF THE INVENTION inhibitor, acts by interfering with the metabolic pathway of 0002 Repetitive chronic condition or behavior is a com alcohol. Normally, alcohol is metabolized to acetaldehyde, mon phenomenology of a closely related array of disorders which in turn is eliminated by oxidation to acetic acid by the often grouped under compulsive obsessive impulsive spec enzyme aldehyde dehydrogenase. Disulfiram inhibits alde trum disorders. Even though these disorders are scattered hyde dehydrogenase and thereby prevents oxidation of alco across the fourth edition of the Diagnostic Statistical Manual hol-generated acetaldehyde to acetic acid. Alcohol consump (DSM IV), published by the American Psychiatric Associa tion during disulfiram treatment, however, leads to the tion, they share common pathogenic features associated with accumulation of acetaldehyde, inducing unpleasant side-ef aberrant sensitivity of the dopamine receptors to dopamine in fects. Because disulfiram does not reduce craving for alcohol, the cortico-mesolimbic system of the brain. These chronic Success with the drug depends on a high level of patient repetitive behaviors may manifest in forms that are physical motivation since patients who wish to drink can simply stop (e.g., characterized by compulsive activity), mental (e.g., taking the drug. Naltrexone, a classical opiate antagonist, obsessive recurrent thoughts), psychological (e.g., Substance appears to act by reducing alcohol craving in abstinent or alcohol abuse), or pathological (e.g., excessive gambling, patients; the drug, however, is hepatotoxic and causes side commission of sexual offenses, etc.). effects that often require medical intervention. Acamprosate, 0003. Of the various disorders associated with chronic a recently approved drug, is thought to act by modulating repetitive behaviors, alcohol abuse and dependence are rec glutamatergic systems. It only has moderate efficacy and has ognized as major public health issues in industrialized yet to gain traction in the U.S. nations. It has been estimated that in the United States alone, 0008 Further it is not necessary that repetitive behavior be as much as 11 to 15 million people may be dependent on or associated with substance or alcohol abuse. Repetitive behav abusing alcohol. In the U.S., alcohol dependence accounts for ior can also manifest itself in the form of recurrent or persis 9% of the intensive care unit (ICU) admissions, about 85,000 tent thoughts, images, impulses, or mental acts performed to deaths per year, and costs the economy as much as S100 relieve anxiety, neutralize intrusive neurogenic signals, or billion per year. relieve distress. As with alcohol and Substance dependence, 0004. It has also been noted that physicians have an unfa patients with this type of disability have a poor overall quality vorable attitude towards alcoholism and alcoholics which of life and experience significant impairment in academic often impacts the treatment of the disease. Physicians' apathy functioning, work performance, and relationships. It is esti towards alcoholism is Surprising in view of the recognition by mated to be the tenth leading cause of disability in the world. various National Institutes of Health organizations and the 0009. Accordingly, there is a need in the art for composi American Medical Association of alcoholism as a primary tions that are safe and effective for the therapeutic manage chronic disease which is often progressive and fatal. Alcohol ment of chronic repetitive behavior, e.g., alcohol dependence, dependence is co-morbid with a variety of psychiatric disor on a chronic basis. The present invention satisfies this and ders such as anxiety, depression, bipolar mania, Schizophre other needs. nia, etc. 0005 Physicians often perceive alcoholism as a moral SUMMARY OF THE INVENTION failure rather than a disease and tend to have pessimistic view 0010. The present invention provides novel compositions of the effectiveness of treatment interventions. Other barriers comprising a combination of a 5-HT receptor antagonistand that physicians face are more practical than attitudinal. Lack a selective dopamine D receptor antagonist for the treatment of an appropriate reimbursement system for alcohol screen of chronic repetitive behavior associated with abnormal sen ing, assessment, and treatment, limited time and resources, sitivity of dopamine receptors to dopamine in the cortico lack of provider training, and an inadequate referral system mesolimbic system of the brain. The repetitive chronic con all hampera physician's efforts to help these patients. ditions may be physical (e.g., characterized by a compulsive 0006. A craving is a powerful urge to repeatedly drink and behavior), mental (e.g., obsessive thoughts), psychological is central to abstinence from alcohol or maintenance of alco (e.g., characterized by Substance abuse or dependence such as holism. Alcohol induces craving by reinforcing the stimula alcohol dependence), or pathological (e.g., characterized by tory and rewarding effects of alcohol via a neurological pro gambling, commission of sexual offenses). cess that involves the interplay between 5-HT receptors on 0011. Of the various disorders associated with chronic the mesolimbic arm of the dopamine pathway, dopamine, and repetitive behaviors, alcohol abuse and dependence are rec US 2010/0113483 A1 May 6, 2010 ognized as major public health issues in industrialized second amount of a selective dopamine D receptor antago nations. It has been estimated that in the United States alone, nist, wherein the amounts of the antagonists are Sufficient to as much as 11 to 15 million people may be dependent on or treat the Subject, and instructions on the use of the antago abusing alcohol. In the United States, alcohol dependence nists. accounts for 9% of the intensive care unit (ICU) admissions, 0020. In a further aspect, the present invention provides a about 85,000 deaths per year, and costs the economy as much pharmaceutical composition comprising a first amount of a as S100 billion per year. Furthermore, it is not necessary that 5-HT receptor antagonistanda second amount of a selective repetitive behavior be associated with substance or alcohol dopamine D receptor antagonist. abuse. Repetitive behavior can also manifest itself in
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