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TRPV1: Not Dead Yet 78 Potential Opportunities: • Development by different routes of administration (e.g., topical). • Development of short half-life antagonists. • Development of antipyretic + TRPV1 antagonist combination. • Development of TRPV1 antagonists in primary indications (e.g., OA). • One compound previously in development (GSK’s SB-705498) did not induce hyperthermia in patients treated with 400mg of the drug. Amgen presentation, Arrowhead Pain Conference 2008 © Defined Health, 2009 Pain Insight Briefing
TRPV1 Antagonist Pipeline Compound AZD 1386 MK 2295 JTS 653 Vanilloid receptor antagonists Ion channel modulators Small molecule therapeutics Transient receptor potential vanilloid 1 cation channel antagonists TRPV antagonists TRPV cation channel inhibitors TRPV1 antagonists TRPV1 antagonists TRPV1 cation channel inhibitors TRPV1 receptor antagonists Vanilloid 1 receptor antagonists Vanilloid receptor antagonists Vanilloid receptor antagonists Vanilloid receptor antagonists TRPV1 cation channel inhibitors GRC 6211 SB 705498 AMG 517 TRPV1 cation channel antagonists 79 Adis R&D Insight Developer AstraZeneca Merck/Neurogen Japan Tobacco Renovis/Pfizer Hydra Biosciences Amphora Abbott Sanofi-Aventis Purdue Pharma Diver Drugs Eli Lilly J & J Traxion AmorePacific/Schwarz Neurogen/Merck Novartis Pharmeste Mochida//Wyeth Glenmark/Eli Lilly Amgen Amgen Phase Phase-II Phase-II Phase-I Phase-I Preclinical Preclinical Preclinical Preclinical Preclinical Preclinical Preclinical Preclinical Preclinical Preclinical Preclinical Preclinical Preclinical Research Discontinued-II Discontinued-II Discontinued-I Discontinued- Preclinical © Defined Health, 2009 Pain Insight Briefing Indications Gastro-oesophageal reflux, Pain Pain Overactive bladder, Pain Pain, Urinary incontinence Asthma, HTN, Inflammation, Kidney disorders, Lung disorders, Osteoporosis, OAB, Pain CNS disorders, Metabolic disorders, Pain Pain Inflammation, Neuropathic pain Pain Inflammation, Pain Inflammation, Pain, Urinary incontinence Cough, Pain Pain Pain Pain Neuropathic pain Neuropathic pain, Urinary incontinence Pain Cystitis, Dental pain, Neuropathic pain, Urinary incontinence
Page 1 and 2:
Game Changing Plays in the Pain Mar
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Our Disclaimer 3 The information in
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Everyone Hurts “Pain is whatever
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It’s A Big Market with a Few Domi
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$ Millions But Few “Big Pharma-Si
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Pain Historically: Drug Delivery ha
Page 13 and 14:
It’s Getting Tougher Labopharm La
Page 15 and 16:
The Risk : Reward Profile for Novel
Page 17 and 18:
Current Standard of Care for Pain
Page 19 and 20:
Leaving Plenty of Unmet Need to Be
Page 21 and 22:
In the Meantime, Let’s Teach Old
Page 23 and 24:
A Better NSAID: NicOx • Naproxcin
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A Better NSAID: NicOx 25 Company pr
Page 27 and 28: A Better NSAID: Pozen / AstraZeneca
Page 29 and 30: The First-to-Market Topical NSAIDs
Page 31 and 32: Even So, Flector is Expected To Be
Page 33 and 34: Now We Have a Patch and a Gel Volta
Page 35 and 36: The Need is Clear 35 © Defined Hea
Page 37 and 38: Progenics / Wyeth: Making Opioids M
Page 39 and 40: Adolor / Pfizer: Making Opioids Mor
Page 41 and 42: Like All Things CNS, It’s Not So
Page 43 and 44: A New, and Better Opioid from J&J /
Page 45 and 46: A New, and Better Opioid from J&J /
Page 47 and 48: Opioid Abuse Deterrence 47 © Defin
Page 49 and 50: King Pharmaceuticals: Making Big Be
Page 51 and 52: But Also Significant Hurdles • Te
Page 53 and 54: The Technologies are Not the Proble
Page 55 and 56: The Real Issue is Risk Management
Page 57 and 58: Fentanyl: Again, REMS is the Big Re
Page 59 and 60: Lessons from Fentora 59 What the FD
Page 61 and 62: For Some Mechanisms, the US Regulat
Page 63 and 64: FAAH Pipeline 63 Compound SSR 10101
Page 65 and 66: FAAH Pipeline KDS-4103, acquired by
Page 67 and 68: Addressing the Big Problem 67 >50%
Page 69 and 70: New MOA Challenges 69 NeuroDiscover
Page 71 and 72: New MOA Challenges 71 The identific
Page 73 and 74: TRPV1 • The transient receptor po
Page 75 and 76: TRPV1: Target for Novel Analgesics
Page 77: TRPV1 Antagonists: Hot … Too Hot
Page 81 and 82: TRPV1 Antagonist Pipeline 81 Compou
Page 83 and 84: TRPV3: Hopeful, But Too Early to Te
Page 85 and 86: Good Phase III Data, An Accepted ND
Page 87 and 88: Pfizer Pursuing Multiple Chronic Pa
Page 89 and 90: Concerning, but Transient Adverse E
Page 91 and 92: Will NGF for Pain Be Like TNF is fo
Page 93 and 94: Repurposed anti-TNF Antibodies for
Page 95 and 96: What’s Next for Pain? • Continu
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