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(12) Patent Application Publication (10) Pub. No.: US 2011/0065628A1 Johnson Et Al

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(12) Patent Application Publication (10) Pub. No.: US 2011/0065628A1 Johnson Et Al US 2011 0065628A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2011/0065628A1 Johnson et al. (43) Pub. Date: Mar. 17, 2011 (54) MEDICATION COMBINATIONS FOR THE Related U.S. Application Data TREATMENT OF ALCOHOLISMAND DRUG (60) Provisional application No. 60/966,265, filed on Aug. ADDCTION 27, 2007. Publication Classification Inventors: (75) Bankole A. Johnson, (51) Int. Cl. Charlottesville, VA (US); Nassima A63L/485 (2006.01) Ait-Daoud Tiouririne, A6II 3/55 (2006.01) Charlottesville, VA (US); Wendy J. A6II 3/55 (2006.01) Lynch, Charlottesville, VA (US) A 6LX 3/59 (2006.01) A63/496 (2006.01) A6II 3/56 (2006.01) (73) Assignee: UNIVERSITY OF VIRGINA A638/02 (2006.01) PATENT FOUNDATION, A6IP 25/30 (2006.01) Charlottesville, VA (US) A6IP 25/32 (2006.01) A6IP 25/36 (2006.01) A6IP3/04 (2006.01) (21) Appl. No.: 12/675,486 (52) U.S. Cl. .......... 514/1.1: 514/282: 514/215: 514/221; 514/259.41: 514/253.04: 514/253.07: 514/171 (22) PCT Fled: May 20, 2008 (57) ABSTRACT The present invention provides for the use of combinations of (86) PCT NO.: PCT/USO8/64232 drugs to treat addictive disorders. More specifically, the present invention provides compositions and methods for S371 (c)(1), treating disorders using combinations of drugs such as topi (2), (4) Date: Feb. 26, 2010 ramate, ondansetron, and naltrexone. Patent Application Publication Mar. 17, 2011 Sheet 1 of 15 US 2011/0065628A1 3 Mean :::: EEEE EEE D',ay E::::::: :::: B EEEE :::: 1 EEE E::: :: O EEE Plac Ond 1 Ond 4 Ond 16 Plac Ond 1 Ond 4 Ond 16 Start of double blind End of study Placebo (Plac) geton 1 ug/kg b.i.d. n Ondansetron 4 g/kg I Ondansetron 16 ug/kg b.i.d. b.i.d. (Ond 4) (Ond 16) FIG. 1A Patent Application Publication Mar. 17, 2011 Sheet 2 of 15 US 2011/0065628A1 3 i Mean :::: :::: I Drinks 1 EEE :::: Day 2 EEE :::: :::: S ::::: EEE: 1 :::: EEE :::: E :::: EEE O EEE Plac Ond 1 Ond 4 Ond 16 Plac Ond 1 Ond 4 Ond 16 Start of double blind End of study Placebo (Plac) --: 25,Ondansetron 1 ug/kg b.i.d. Ondansetron 4 ug/kg I Ondansetron 16 g/kg b.i.d. b.i.d. (Ond 4) (Ond 16) F.G. 1B Patent Application Publication Mar. 17, 2011 Sheet 3 of 15 US 2011/0065628A1 0.3 Mean 0.2 Log CDT 0.1 Ratio -0.0 -0. -0.2 -0.3 -0.4 Plac Ond 1 Ond 4 Ond 16 Ondansetron doses in lug/kg b.i.d. Placebo (Plac) ndeton 1 g/kg b.i.d. Ondansetron 4 ug/kg Ondansetron 16 g/kg b.i.d. b.i.d. (Ond 4) (Ond 16) FIG. 2A Patent Application Publication Mar. 17, 2011 Sheet 4 of 15 US 2011/0065628A1 Mean CDT Ratio Plac Ond 1 Ond 4 Ond 16 Ondansetron doses in g/kg b.i.d. Placebo (Plac) Ondansetron 1 ug/kg b.i.d. (Ond 4) Ondansetron 4 g/kg H Ondansetron 16 ug/kg b.i.d. b.i.d. (Ond 4) (Ond 16) FIG. 2B Patent Application Publication Mar. 17, 2011 Sheet 5 of 15 US 2011/0065628A1 6 O Group Mean -0- 0. Naltrexone 4O -- 0.3 Naltrexone -0- 1.0 Naltrexone 2O -- 3.0 Naltrexone O -2O AQ S S S S) (S 19 QS QS SS AS S S AS as es 1S AS Time (10 minute time blocks) FIG. 3 Patent Application Publication Mar. 17, 2011 Sheet 6 of 15 US 2011/0065628A1 1O 9 Mean 8 drinks/ 6 drinking 5 day 4 \ 3 2 1 O O 1 2 3 4 5 6 7 8 ? A Study Weeks Baseline Start of double-blind Ondansetron 4 u g/kg b.i.d. + Naltrexone 25 mg b.i.d. group -O-Placebo group FIG. 4A Patent Application Publication Mar. 17, 2011 Sheet 7 of 15 US 2011/0065628A1 12 11 1O Mean 9 drinks/ 8 drinking 7 day 6 5 4 3 2 1. O O l 2 3 4 5 6 7 8 A A Study Weeks Baseline Start of double-blind Ondansetron 4 u g/kg b.i.d. + Naltrexone 25 mg b.i.d. group -O-Placebo group FIG. 4B Patent Application Publication Mar. 17, 2011 Sheet 8 of 15 US 2011/0065628A1 || || || 1 1 2 3 4 5 6 7 8 9 1 0 1 1 12 Week of Study - A - Placebo -O-2.5 mg Rit - a 5.0 mg Rit FIGS Patent Application Publication Mar. 17, 2011 Sheet 9 of 15 US 2011/0065628A1 Alcohol Dependent patients N=360 Early Onset Alcoholics Late Onset Alcoholics (EOA) N=180 (LOA) N=180 •Alcoholism onsets 25 years •Alcoholism onset >25 years •High family history of alcoholism •Less family history of alcoholism in 1st degree relatives in list degree relatives "Antisocial behaviors and symptoms •Few antisocial behaviors and symptoms Cognitive Behavioral Therapy Cognitive Behavioral Therapy Placebo Ondansetron Ondansetron -- Ondansetron Ondansetron Placebo Placebo Naltrexone Placebo Naltrexone Naltrexone Naltrexone Placebo N=45 N=45 N=45 F.G. 6 Patent Application Publication Mar. 17, 2011 Sheet 10 of 15 US 2011/0065628A1 Study years Subject Enrolled Completed Effect of Naltrexone/Topiramate on Alcohol Consumption o E p e Vehicle 5 Top 10 Top Nalf Naf10 Top 1 Nal -24 5 Top FIG. 8 Patent Application Publication Mar. 17, 2011 Sheet 11 of 15 US 2011/0065628A1 Efferents to Frontal Cortex 8 HippocampuS Efferents to Hippocampus 5HT3 receptors 3- endorphins Serotonin 5HT3 receptor facilitated GABA interneurons Dopamine Afferent from the Hippocampus to the N. Accumbens Patent Application Publication Mar. 17, 2011 Sheet 12 of 15 US 2011/0065628A1 7 6 Ethanol intake 5 (-12%) (g/kg) w 3 2 1 2 3 4. 5 6 7 Session FIG 10A Ethanol intake (glkg) Session FIG 10B Patent Application Publication Mar. 17, 2011 Sheet 13 of 15 US 2011/0065628A1 6 (1%) Ethanol 5 W intake (g/kg) 4 3 2 1 2 3 4. 5 6 7 Session FIG 10C 7 6 (17%) Ethanol intake 5 w (g/kg) 3 2 1 2 3 4. 5 6 7 Session FIG 10D Patent Application Publication Mar. 17, 2011 Sheet 14 of 15 US 2011/0065628A1 7 6 Ethanol 5 - intake (g/kg)Ik 4. - (28%) 3 - W Session FIG 10E Patent Application Publication Mar. 17, 2011 Sheet 15 of 15 US 2011/0065628A1 Prefrontal cortex Arnygdala GLU Serotonin Lateral septum Cholinergic Modulatory Input Hippocampus. Excitatory input From Raphe. Nuclei From PPTg and LDT.g | ExcitatoryGU Input CB1R Enkephalin Dopamine inhibitory input (D1, D2, D3) From Nucleus Ya GABA Arcuatus Inhibitory Input Neuron h GABA Neuron 5-HT3-R Receptors Mu a 3 GABA inhibitory Feedback N GABA Neuron REINFORCEENT Wentral Tegmental Area H (WTA) — H Nucleus(nACC) Accumbens — FIG 11 US 2011/0065628 A1 Mar. 17, 2011 MEDICATION COMBINATIONS FOR THE targeted towards correcting or ameliorating the underlying TREATMENT OF ALCOHOLISMAND DRUG abnormalities. Because these abnormalities involve several ADDICTION neurotransmitters, combinations of medications targeting specific systems may yield better clinical outcomes than CROSS REFERENCE TO RELATED treatment of only one affected pathway would alone. Hence, APPLICATIONS obtaining optimal treatment matching combinations for vari 0001. This application is entitled to priority pursuant to 35 ous types of alcoholic remains an important research goal. U.S.C. S 119(e) to U.S. provisional patent application No. 0006 Alcohol abuse and dependence are widespread and 60/966,265, filed on Aug. 27, 2007. The entire disclosure of it is estimated that 14 million American adults abused alcohol the afore-mentioned patent application is incorporated herein or were dependent on it in 1992 and that approximately 10% by reference. of Americans will be affected by alcohol dependence some time during their lives. Alcohol dependence, characterized by STATEMENT REGARDING FEDERALLY the preoccupation with alcohol use, tolerance, and with SPONSORED RESEARCH ORDEVELOPMENT drawal, is a chronic disorder with genetic, psychosocial, and environmental factors influencing its development and mani 0002 This invention was made in part with United States festations. Studies have demonstrated the significance of Government support under National Institutes of Health opioids (i.e., beta-endorphin), dopamine (DA), serotonin Grant Nos. AAO12964 and AA13074. The United States Gov (5-HT), Y-amino-butyric acid (GABA), and glutamate for the ernment has certain rights in the invention. development and maintenance of alcohol dependence. To date, most pharmacotherapy trials have focused on single FIELD OF THE INVENTION pharmacological agents. However, because of the failure to 0003. The present invention relates generally to the use of find consistent results with these drug therapies, investigating combination therapies to treat addiction-related diseases and the efficacy of combining drugs that target multiple neu disorders and impulse control disorders, particularly alcohol rotransmitter systems or genes is perhaps more important to related diseases and disorders. the development of future pharmacotherapies for treatment of alcohol dependence and treatment of other addictive disor BACKGROUND ders and impulse control disorders. 0004 Neuroscientific advances have greatly increased the 0007 Various medications and behavioral therapy have understanding of the pharmaco-behavioral effects of various been used to treat alcohol dependence. The neuronal targets neurotransmitter systems in the acquisition and maintenance of alcohol include many neurotransmitter systems and the of alcohol dependence. Medications that interact either molecules participating in or regulating the systems, includ directly or indirectly with neurotransmitters that modulate ing GABA, glutamate, DA, opioids, and serotonin (for a cortico-mesolimbic dopamine (CMDA) neurons have been review see Johnson, 2004, Expert Opin. Pharmacother. 5:9: central to most pharmacological strategies in the last decade 1943-1955).
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