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25 Years After Prozac

25 YEARS AFTER PROZAC ANTIDEPRESSANTS STILL OFFER HIGH MARKET POTENTIAL Last year marked the 25th anniversary of the U.S. launch of the iconic antidepressant, Prozac. This medical breakthrough led to a series of new medications for people experiencing depression and opened the door to a blockbuster era for depression drugs. During its peak in 2003, the branded depression drug market was worth nearly $15 billon, but by 2012, as many of blockbuster antidepressants hit patent cliffs and generic competition increased, the market lost almost a third of its value, dropping to $9,560 billion, and with a further expected drop to $7.207 billion by 2019. Despite this decline in sales of the former blockbusters, the high global incident rate of depression (the leading cause of disability) and low market penetration in some areas, presents a variety of opportunities. Such opportunities exist for new market players and treatments, including three notable drugs in phase Il of the pipeline with mechanisms that significantly differ from their predecessors. DEPRESSION DRUG TIMELINE (U.S. LAUNCHES) TITLE? :::.. 350 million people worldwide have depression 1980s 1988 Prozac 1990s 9% of the U.S. population has depression • 1991 Paxil • 1992 Zoloft • 1998 Celexa (1989 European launch) • 1994 Effexor • 1994 Remeron 2000s • 2002 Lexapro 2004 Cymbalta Less than 50% of depressed people globally get treatment 2008 Pristiq 2010s 2011 Viibryd 2013 Brintellix (forecast to make sales of $1.739 billion by 2019) In some countries, less than 10% get treatment 2013 Fetzima SOURCE: SOURCE: THOMSON REUTERS SPOTLIGHT ON DEPRESSION WORLD HEALTH ORGANIZATION AND CENTER FOR DISEASE CONTROL THOMSON REUTERS CORTELLIS™ COMPETITIVE INTELLIGENCE WORLDWIDE SALES OF BRANDED ANTIDEPRESSANT MARKET 15 12 9. 6. 3 2003 2012 2019 REPORTED SALES FORECAST SALES SOURCE: THOMSON REUTERS SPOTLIGHT ON DEPRESSION THOMSON REUTERS CORTELLIS COMPETITIVE INTELLIGENCE ANTI-DEPRESSANT INVENTIONS 1988-2013 1988 1989 1990 New 2-aryloxy-propan-amine New optically active form of citalopram and prepn. of racemic or optically active citalopram by ring closure New 2-aryloxy-propan-amine derivs. useful as inhibitors of derivs. useful as inhibitors of serotonin and nor:epinephrine serotonin and nor:epinephrine uptake uptake of a substd. benzonitrile 1992 New 1-(1,4-bi:phenyl-methyl) benzimidazole(s) as 1992 1993 Treatment of depression using S (plus) fluoxetine gives reduced toxic and psychological effects, rapid onset of action and high angiotensin Il antagonists for treating hypertension, coronary insufficiency, angina gastrointestinal disorders, chronic bronchitis, Optically pure methylol-fluoro- phenyl-piperidine deriv. prepn. by selective biochemical hydrolysis of corresp. acid, isomer sepn. and redn., used as intermediate for antidepressant depression, Alzheimer's and Parkinson's response rate disease, etc. paroxetine 1996 New (piperidinyl-, pyrrolidinyl- or azetidinyl-methyl)indole or derivs. are serotonin agonists used to treat depression, anxiety, eating disorders, drug abuse, pain, migraine 1994 1996 Controlled release of phenyl:ethylamine deriv. antidepressant using dosage form contg. poly:alkylene oxide, New paroxetine hydrochloride anhydrate free of propan-2-ol useful for treating medical disorders e.g. alcoholism, anxiety, depression, anorexia, obesity and pre-menstrual syndrome cellulose or maltodextrin polymer as displacement compsn. 1998 Citalopram preparation, useful as antidepressant by reacting e.g. a 5-alkoxycarbonylphthalide with Grignard reagents of 4-halo-fluorophenyl, then 3-halo-N,N-di:methyl-propylam ine, ring closure and conversion to 5-cyano derivative 1997 1998 Encapsulated, extended release Citalopram preparation, useful as antidepressant by reacting e.g. 4-fluorophenyl:magnesium bromide with 5-cyano:phthalide, reducing oxo group, ring closing hydroxy compound and alkylating formulation of venlafaxine used as anti-depressant, providing better control of blood plasma levels than conventional formulations 1998 Fluoxetine enteric pellet comprising fluoxetine and excipients, 1999 2000 optional separating layer, enteric layer of hydroxy:propyl methyl:cellulose acetate succinate and excipients and optional finishing layer Preparation of selective serotonin reuptake inhibiting citalopram used as antidepressant Composition useful for treating depression, obesity, epilepsy and Alzheimer's disease comprises (-)-venlafaxine 2000 2000 2000 Preparation of citalopram used as antidepressant by dehydrating new oxazoline compound or thermally cleaving new thiazoline compound New crystalline citalopram base, useful as an antidepressant and as intermediate in the production of crystalline citalopram salts Preparation of citalopram as antidepressant drug and for treating dementia and cerebrovascular disorders comprises reaction of a new intermediate with Preparation of citalopram in high yields and purity comprises reacting isobenzofuran compound and cyanide in the presence of palladium catalyst and e.g.copper ions Preparation of citalopram by reaction of a halo-derivative 3-(N,N-dimethylamino)propyl magnesium halide with a cyanide source in the presence of a nickel catalyst SOURCE: DERWENTO WORLD PATENT INDEX THOMSON® INNOVATION ANTIDEPRESSANTS IN THE PIPELINE DRUG, DEVELOPER AND MECHANISM OF ACTION SALES INDICATIONS UNDER FORECASTS DEVELOPMENT ALKS-5461 (samidorphan plus buprenorphine), Designed as a non-addictive kappa opioid antagonist for refractive depression. First sales are forecast for 2016, Phase III development planned to Alkermes start in early 2014 • mu opioid receptor antagonist (samidorphan); kappa opioid antagonist, ORL1 partial agonist and mu opioid partial agonist (buprenorphine) rising to $350 million by 2019 RG-7090, Roche First sales are forecast for Anticipated Phase II for depression and fragile X • mGluR5 antagonist $107.3 million by 2016 Phase II for depression Sales are forecast from 2017, reaching $679.2 million by 2019 RG-1578, Roche • metabotropic glutamate 2/3 receptor (mGluR2/3) antagonist SOURCE: THOMSON REUTERS SPOTLIGHT ON DEPRESSION THOMSON REUTERS CORTELLIS COMPETITIVE INTELLIGENCE DEPRESSION DRUG PATENT FILING THE MOST ACTIVE PARTIES IN FROM 2003 TO 2013 DEPRESSION PARTNERING H Lundbeck A/S ● GlaxoSmithKlyne plc • Eli Lilly &Co • Cephalon Inc ● Neuralstem Inc O Bristol-Myers Squibb Co O Pfizer AstraZeneca Merck &Co Cortex Pharmaceuticals Inc 124% increase 50% decrease SOURCE: SOURCE: DERWENT WORLD PATENT INDEX THOMSON REUTERS SPOTLIGHT ON DEPRESSION THOMSON INNOVATION THOMSON REUTERS RECAP USD BILLIONS 00

25 Years After Prozac

shared by MM19130 on Jul 09
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25 Years After Prozac is an infographic illustrating a timeline from the 1988 launch of Prozac to a current outlook at depression prevalence rates and drug, patent and deal landscapes.

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