INTER AMERICAN DRUG ABUSE CONTROL COMMISSION C I C A D

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INTER AMERICAN DRUG ABUSE CONTROL COMMISSION C I C A D Secretariat for Multidimensional Security FORTY SIXTH REGULAR SESSION November 18 20, 2009 Miami, Florida OEA/Ser.L/XIV.2.46 CICAD/doc.1760/09 11 November 2009 Original: Spanish PROGRESS IN DEVELOPING MEDICATIONS AND VACCINES FOR DRUG ADDICTION TREATMENT DR. IVAN MONTOYA

Progress in Developing Medications and Vaccines for Drug Addiction Treatment Iván D. Montoya, M.D., M.P.H. Acting Deputy Director, Division of Pharmacotherapies and Medical Consequences of Drug Abuse NIDA

Addiction Chronic disease Compulsive behavior of drug use Brain changes Genetic/environmental risk factors Medical, psychological and social consequences Prevetable Treatable Frequently with relapses

DA D2 Receptor Availability Dopamine D2 Receptors are Lower in Addiction DA DA Cocaine DA DA DA DA DA DA DA DA DA DA Reward Circuits Non-Drug Abuser Alcohol DA DA DA DA DA DA Heroin Control Addicted Reward Circuits Drug Abuser

Illicit Drug Addiction Millions of People NSDUH, 2006

Rationale for Medications and Vaccine Research Public health problems Limited efficacy of psychotherapies New knowledge about the effects of illicit drugs and pathophysiology of addictions New pharmacological targets New biomarkers Pharmacogenetics New molecules, medications and vaccines

The NIDA Medications Development Program Congressional Mandate to NIDA March, 1990 Establish a national program on biological and pharmacological approaches to heroin and cocaine addiction treatment. Develop a close working relationship with the pharmaceutical industry. Conduct studies to gain approval of new medications for addiction treatment. Work with FDA to assure that efficacy of compounds is expeditiously evaluated and approved.

The NIDA Medications Development Program Partnership Industry-Academia-Govt. Screening Preclinical Profiling & Lead Optimization Preclinical Safety Phase 1 Safety Phase 2 Activity Dose Phase 3 Efficacy NDA Approval FDA

Pharmacotherapy Approaches P P Abuse Dependence / Addiction USE P P P SIDs Intoxication Withdrawal Delirum Psychosis Anxiety Mood Sleep Sexual P Medical Psychological Social Sequelae

The NIDA Medications Development Program Four NDA approvals: Levo-Alpha Acetyl Methadol (LAAM) Buprenorphine Buprenorphine/naloxone Naltrexone In late-stage development: Lofexidine Nicotine vaccine

Opioid Addiction Methadone Buprenorphine Naltrexone LAAM Clonidine Lofexidine

Methadone or Buprenorphine Compared to heroin users who are not in treatment, patients in treatment show: death rates criminal activity / incarceration employment needle sharing HIV infection rates Advantage of buprenorphine: Safer in overdose situations (due to partial agonist activity)

Total number of patients receiving a prescription for Subutex or Suboxone from U.S. outpatient retail pharmacies, Years 2003-2008 SDI Total Patient Tracker, Extracted 3/09 Patients 500,000 450,000 400,000 350,000 300,000 250,000 200,000 150,000 100,000 50,000 SUBOXONE SUBUTEX 0 2003 2004 2005 2006 2007 2008 Years File: TPT 2009-347 SAMHSA 3-6-09 Subutex Suboxone.xls

Cocaine

Cocaine Medications Evaluated Phase I Phase II Screen Phase II Phase III Carnitine/CoQ Amantadine Selegiline TS Cocaine Vaccine Baclofen Disulfiram Cyclazocine Donepezil Bupropion Tolcapone Gabapentin Cabergoline Modafinil Gingko Desipramine Metyrapone Hypericum celebrex Dextroamphetamine Lamotrigine Levodopa/Carbidopa Olanzapine Ondansetron Paroxetine Pentoxifylline Piracetam Pramipexole Riluzole Sertraline Tiagabine Valproate Disulfiram Enadoline Hydergine Mazindol Methylphenidate Naltrexone Pemoline Pergolide Phenytoin Propranolol Reserpine Risperidone Selegiline IR Valproate Modafinil Baclofen Naltrexone Desipramine Buprenorphine Vaccine

Vigabatrin for Cocaine Addiction Abstinence During Last 3 Weeks of Tx Failures Placebo 49 (92.5%) Successes 4 (7.5%) 3.7 x Vigabatrin 36 (72%) 14 (28%) P = 0.009 (Chi-square test)

Methamphetamine

Bupropion for Methamphetamine Addiction Abstinence During Last 3 Weeks of Tx Failures Placebo 68 (94.4%) Successes 4 (5.56%) 3.2 x Bupropion 65 (82.3%) 14 (17.7%) P = 0.02 (Chi-square test)

Immunotherapies Vaccines Antibodies

Immunotherapy Development Program Preclinical Studies anti-pcp mab anti-methamphetamine mab anti-mdma mab anti-cocaine mab Clinical Studies Anti-Nicotine vaccine Anti-Cocaine vaccine

Capillary Blood Flow Antibodies Mechanism of Action Brain (Owens & Gentry 2002)

Rationale for Immunotherapy against Addictions Drug Use Drug in blood ADDICTION X Blood/Brain Barrier Reward Dopamine Release Receptors in Brain

24 Nicotine Addiction

Nicotine Vaccine

Breaking the Addiction Cycle 26

Proportion of Subjects Quit Each Week: Point Prevalence Stratified by Antibody Levels 45 40 35 TQD TQD All NicVAX Subjects: ITT N=18/61 p=0.0055 % Quit per Week 30 25 20 15 N=12/100 10 5 placebo low Ab high Ab* N=17/140 0 0 5 10 15 20 25 30 35 40 45 50 Study Week *Top 30% by AUC

Cocaine Vaccine

Potential Clinical Applications MAbs Overdoses Prevent brain toxicity Vaccines Aid to quit use Relapse prevention Prevention of brain toxicity Prevention of development of addiction

Summary Medications approved by the FDA for opioid (heroin) addiction (methadone, buprenorphine, naltrexone) Medications under research for cocaine, methamphetamine, and cannabis addiction Immunotherapy (vaccines or antibodies) is a promising approach Nicotine and cocaine vaccines phase III clinical trials in progress