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Pre-conference briefing - 26 November 2007 - Bringing therapies for type II diabetes closer to market
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| 09.20 | Chairman’s opening remarks
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| | Pierre Honoré, Vice President, Strategy and Sourcing, Diabetes Research, Novo Nordisk
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| METABOLIC MILESTONES – NEW TARGETS, MECHANISMS AND THERAPIES |
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| 09.30 | Underscoring the need for new therapies with new mechanisms
- Understanding the network of pathways that work together to regulate plasma glucose levels
- Identifying druggable targets and providing proof-of-concept for a number of mechanisms
- New strategies and programs addressing intractable targets and seeking to agonise enzymatic activity
- New ways of improving insulin sensitisation with improved tolerability
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| | Håkan Wennbo, Vice President Portfolio Strategy - Diabetes and Obesity, Astrazeneca R&D
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| IDENTIFYING DRUGGABLE TARGETS |
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| 10.00 | Targeting the Sodium Glucose Transporter II and developing selective inhibitors
- The therapeutic rationale for inhibiting SGLTII
- Outstanding challenges of identifying molecules capable of inhibiting the SGLTII protein
- SLGTII inhibitor working in combination with existing drugs due to independent glucose-lowering mechanisms
- Data reporting from ongoing Phase trials
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| | Chari Smith, Program Lead, SGLT2, Department of Biochemical and Analytical Pharmacology,, Glaxosmithkline
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| 10.30 | Morning coffee
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| 11.15 | Glucokinase Activators in Diabetes Management: The discovery and pre-clinical evaluation of Glucokinase Activators (GKAs)
- GKA acting as allosteric activators increasing the catalytic effectiveness of glucokinase enzymes
- Increasing glucose affinity whilst maintaining natural glucose sensing characteristics
- In vitro characteristion and in vivo mechanism of action
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| | Matthew Coghlan, Candidate Drug Delivery Team Leader, Diabetes and Drug Discovery,, AstraZeneca
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| 11.45 | Current clinical development of gastro intestinal hormones as treatments for diabetes: GLP-1 receptor agonists and Exenatide
- Therapeutic approaches for using the incretin system through GLP-1 receptor agonists
- What do these compounds add to current therapies? Comparing pre-clinical with that of clinical data
- Overview of clinical efficiency of Exenatide and GLP-1 receptor agonists
- New developments for long-acting drugs
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| | Hubert Chen, Director of Clinical Research, Amylin Pharmaceuticals
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| 12.15 | Panel session: additional Q&A on SGLT2, GKA and GLP-1
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| | Moderator: Pierre Honoré, Vice President, Strategy and Sourcing, Diabetes Research, Novo Nordisk Confirmed: Chari Smith, Program Lead, SGLT2, Department of Biochemical and Analytical Pharmacology,, Glaxosmithkline Confirmed: Matthew Coghlan, Candidate Drug Delivery Team Leader, Diabetes and Drug Discovery,, AstraZeneca Confirmed: Hubert Chen, Director of Clinical Research, Amylin Pharmaceuticals
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| 12.45 | Lunch
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| 14.00 | Current development of long-acting GLP-1 analogs and Liraglutide
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Therapeutic approaches for enhancing incretin action through GLP-1 receptor agonists
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What do these compounds add to current therapies?
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Overview of clinical efficiency in the GLP-1 related drug classes
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Preclinical and clinical studies to determine the glucose land body weight owering efficiency of Liraglutide |
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| 14.30 | GPR119 agonists as potential agents for the treatment of “diabesity”
- GPR119 is a GPCR expressed predominantly in the pancreas and gastrointestinal tract
- Oleoylethanolamide (OEA), a known anorectic agent in rodents, is the most active endogenous agent described thus far (Cell Metab 3, 167 (II006))
- We have identified novel, selective, orally available GPR119 agonists as exemplified by the prototypical PSN63II408 and other compounds
- Studies describing the effects of these GPR119 agonists in various cell models and animal models of obesity and diabetes will be presented
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| | Jim McCormack, Vice President Research and Chief Scientific Officer, Prosidion Ltd. (a subsidiary of OSI Pharmaceuticals Inc.)
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| 15.00 | Afternoon tea
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| 15.30 | Fighting diabetes Type II with ‘expenditure genes’
- Is diabetes Type II a disease or a consequence? Are we treating the symptoms or the disease?
- The paradox; why some obese people do not develop diabetes and why some lean individuals do
- A new approach for identifying genes for diabetes treatment
- A drug versus work-out regime
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| | Itzik Harosh, Chairman and Chief Scientific Officer, ObeTherapy
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| 16.00 | Panel session: additional Q&A on GLP-1, GPR119 and expenditure genes
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| | Moderator: Pierre Honoré, Vice President, Strategy and Sourcing, Diabetes Research, Novo Nordisk Confirmed: Jim McCormack, Vice President Research and Chief Scientific Officer, Prosidion Ltd. (a subsidiary of OSI Pharmaceuticals Inc.) Confirmed: Itzik Harosh, Chairman and Chief Scientific Officer, ObeTherapy
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| COMBINATION PHARMACOTHERAPY |
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| 16.30 | Assessment of the potential use of obesity drugs in the treatment of diabetes
- Obesity as a major driver of diabetes
- Use of dietary-induced obesity rodent models
- Relationship of preclinical results to clinical outcomes
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| 17.00 | Close of pre-conference briefing
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Day one 27th November 2007
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| 09.00 | Chairman’s opening remarks
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| | Michael Cawthorne, Director of Metabolic Research & Professorial Research Fellow, University of Buckingham
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| ANTI OBESITY MARKET AND PRODUCT DEVELOPMENT |
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| 09.10 | Opening presentation: evaluating the defining opportunities in obesity drug development
- Identifying the changing dynamics of obesity drug development
- Pricing and reimbursement, policy and socio-anthropologic factors playing an increasing role in defining the market opportunity
- Who is succeeding and how? Developers and manufacturers navigating the arena
- Lessons learned; key barriers today and in the near future
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| | Michael Cawthorne, Director of Metabolic Research & Professorial Research Fellow, University of Buckingham
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| IMPROVED DRUG DEVELOPMENT USING EXISTING TARGETS AND MECHANISMS |
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| 09.40 | Increased efficacy with Rimonabant: evaluating the novel approach with Cannabinoid 1 receptor
- CB1 signaling linked to nicotinic, dopaminergic and other important pathways
- Current programmatic and clinical developments with Acomplia™
- What next? What does the future hold for drug development?
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| 10.10 | Morning coffee
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| 10.40 | Forthcoming Cannabinoid-1 receptor blockers
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Current wave of small molecules antagonising cannabinoid CB1 receptor
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CB1 signaling linked to nicotinic, dopaminergic and other important pathways
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Current programmatic and pre / clinical developments
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How might a CB-1R antagonist improve on Rimonabant? |
| | Moderator: Michael Cawthorne, Director of Metabolic Research & Professorial Research Fellow, University of Buckingham Confirmed: Shridhar Narayanan, Vice President Biological Research, Glenmark Pharmaceuticals Confirmed: Guy Kennett, Senior Fellow Researcher, Vernalis
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| 11.40 | Future prospects for serotonergic drugs in the treatment of obesity and related metabolic disorders
- The renaissance of pharmaceutical interest in serotonergic approaches to the treatment obesity
- Developing both 5-HT2C agonists and 5-HT6 agonists and antagonists as clinical candidates in obesity
- Discussing the likely clinical benefit of these approaches
- Reviewing the regulatory challenges facing these drugs and their likely potential for commercial success
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| | David Heal, Director and Vistiing Professor of Pharmacology, Department of Pharmacy and Pharmacology, RenaSci Consulting and University of Bath
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| 12.10 | Speed networking
- Meet…move on… meet…move on…meet!
- Exchange business cards with fellow conference delegates, speakers and moderators
- The best 50 minute networking session you’ve ever experienced
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| 13.00 | Lunch
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| 14.00 | Key strategies for effective drug discovery
- Understanding the different requirements and expectations that exist for novel anti-obesity agents
- Discovering the multitude of potential drug targets for obesity
- Identifying the problems inherent in both investigational and approved anti-obesity therapies
- Improvements to enhance the therapeutic potential of novel anti-obesity drugs
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| | Jonathan Arch, Deputy Director of Metabolic Research, Clore Laboratory, University of Buckingham
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| 14.30 | Fostering regulatory approval for furthering obesity drug research and development
- Understanding current guidelines placed on regulating obesity drug development
- Requirements placed on the development program, clinical trial, changing regulatory requirements, methods of evaluating and interpreting data and regulatory interpretations of clinical risk and benefit
- Outlining pathways for the pharmaceutical industry towards accelerated approval
- Ensuring efficacy and safety throughout the regulatory approval process
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| | Douglas Greene, Senior Vice President and Chief Medical Officer, Sanofi Aventis
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| PRE-CLINICAL AND ANIMAL MODELING FOR OBESITY STUDIES |
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| 15.00 | Predictive animal models for pre-clinical testing of drug candidates
- Which rodent models are best for predicting the clinical efficacy of new compounds?
- Which obesity-related cardio-metabolic risk factors can be modeled in rodents?
- Strengths and weaknesses of dietary-induced obesity in rats versus mice
- Validity of a particular rodent model for predicting weight-loss efficacy in the clinic relative to anti-obesity drugs in current use
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| 15.30 | Afternoon tea
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| 16.00 | Panel session: linking animal measurements that can be made in Phase I and IIa
- Animal models linking to measurements that can be made in Phase I and IIa
- Developments within an anorectic or metabolic approach and evaluation of thermogenic drug development
- What is over the horizon for Phase I and 2a studies with Obesity drug development?
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| | Moderator: Michael Cawthorne, Director of Metabolic Research & Professorial Research Fellow, University of Buckingham Confirmed: David Heal, Director and Vistiing Professor of Pharmacology, Department of Pharmacy and Pharmacology, RenaSci Consulting and University of Bath Confirmed: Rob Jones, Director, RenaSci Consultancy Ltd
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| 16.30 | Confirming the presumed mechanism of action using obesity biomarkers
- Current lack of validated biomarkers for obesity-related cardiovascular diseases
- Finding optimal biomarkers; allowing diagnostic criteria for cardiovascular diseases to identify early pathologic processes
- Obesity biomarkers used to confirm the presumed mechanism of action
- Identifying biomarkers with promising properties which require further validation in humans
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| | Ann Taylor, Director and Clinical Lead for Obesity Early Development, Pfizer Global R&D
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| DEVELOPMENT OF BIOMARKERS AND DIAGNOSTIC TOOLS |
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| 17.00 | Close of day one followed by networking drinks
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Day two 28th November 2007
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| 09.00 | Chairman’s opening remarks
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| | David Heal, Director and Vistiing Professor of Pharmacology, Department of Pharmacy and Pharmacology, RenaSci Consulting and University of Bath
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| CNS TARGETS AND OBESITY DRUG DEVELOPMENT |
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| 09.10 | A sustained-release combination of bupropion, a dual dopamine and norepinephrine reuptake inhibitor
- Contrave™ as a unique approach to weight loss based on the understanding of the central nervous system
- Activating central pathways associated with both a reduction in appetite and an increase in the expenditure of energy
- Obtaining longer-term efficacy by combining bupropion it with naltrexone
- Four registration trials evaluating a variety of obesity-related outcome measures.
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| 09.40 | Anti-obesity compounds comprising betahistine
- Betahistamine and its effect on weight management
- Histamine analog agonising histamine H1 receptors and partially agonising H3 receptors
- Side-stepping the side effects encountered by pharma when pursuing novel small molecule H3 antagonists
- Future trials looking into metabolic markers such as plasma lipids, LDL, HDL and so on
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| 10.10 | Taking a re-profiling approach with a CNS directed agent
- Tesofensine’s mixed mechanism allowing it to increase metabolism and reduce the need for food intake
- The triple serotonin, dopamine and noradrenaline reuptake inhibitor proof of safety
- Avoiding mood disorders based on its antidepressant-like serotonin reuptake activity
- Future phase trials in the pipeline and clinical projections
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| | Dieter Meier, Executive Vice President and Chief Medical Officer, NeuroSearch
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| 10.40 | Morning coffee
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| 11.00 | Qnexa™ - combination therapy for weight loss and obesity-related co-morbidities
- Rationale for combination therapy in the treatment of obesity-related metabolic disorders
- Benefit of complementary pharmacology from both a safety and efficacy perspective
- Clinical experience with Qnexa™ to date; efficacy data from Phase II and safety and tolerability profile of a low dose combination therapy
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| | Wesley Day, Vice President, Clinical Development, VIVUS
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| DUAL-ACTING ANTI OBESITY AGENTS |
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| 11.40 | Novel approach in harnessing additive / synergistic effects of adipocyte-, islet- and gut-derived hormones
- An integrated neurohormonal approach representing a promising alternative strategy for the treatment of obesity
- Harnessing naturally-occuring synergies among adipocyte-, islet- and gut-derived signals
- Role of neurohormones in the regulation of food intake and energy expenditure
- Clinical results with pramlintide, an amylin agonist plus preclinical results with amylin, PYY3-36, and leptin
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| | Hubert Chen, Director of Clinical Research, Amylin Pharmaceuticals
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| 11.41 | GUT HORMONES AS ANTI-OBESITY TARGETS
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| 12.10 | Discovery and development of a novel analogue of oxyntomodulin
- Oxyntomodulin has been shown to reduce food intake and body weight in clinical studies
- TKS1225 is a novel, potent and long-acting analogue of oxyntomodulin
- Clinical trials of TKS1225 are expected to start in 2008
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| 12.40 | Lunch
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| 14.00 | Evaluating the potential of PYY as an appetite suppressant
- PYY3-36 and Y2 receptors believed to play a role in inducing satiety
- Clinical experience with PYY3-36 – are the results a durable effect?
- Can the PYY3-36 mechanism make it an ideal candidate for a combination approach?
- Translating current results into something usable for a longer period of time – ongoing Phase 2
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| | Gordon Brandt, Executive Vice President of Clinical Research and Medical Affairs, Nastech Pharmaceuticals
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| 14.30 | Agonising Y2 and Y4 receptors with TM30338 synthetic peptide analog
- Administering PYY3-36 and pancreatic polypeptides to address the Y4 receptor
- Advantages of hitting two satiety signals at the same time
- Phase 2 trials further qualifying the pathway and target as well as the pharmacology of the target
- Preparing for the Phase 2b/2I clinical programme
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| PERIPHERALLY-ACTING ANTI OBESITY AGENTS |
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| 15.00 | Afternoon tea
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| 15.30 | A dual-mechanism approach to inhibiting anti-obesity drug targets
- A method of ramping up metabolism without a concomitant increase in appetite
- Increasing the activity of the lipase enzyme implicated in the transport and metabolism of triglycerides
- Viability of targeting both the adipose triglyceride lipase pathway as well as phophosinositide 3-kinase
- Elucidating the exact mechanism of Adyvia
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| ENZYMES AS DRUG TARGETS |
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| 16.00 | Panel session: pros and cons of brain receptors, gut hormones and metabolic targets
- Central targets have given effective drugs, but gut peptides and peripheral metabolic targets are attractive
- What is working and what is not? Is there a need for novel approaches?
- Considerations of feasibility, drug delivery, metabolic benefits and long term efficacy
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| | Moderator: David Heal, Director and Vistiing Professor of Pharmacology, Department of Pharmacy and Pharmacology, RenaSci Consulting and University of Bath Confirmed: Gordon Brandt, Executive Vice President of Clinical Research and Medical Affairs, Nastech Pharmaceuticals
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| 16.30 | Close of conference
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