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Innovation Driven Discovery Discovery Chemistry & Drug Design
Day 1 Stream 1 R&D Models For The Future
Polypharmacology: new opportunities for open innovation
Virtual R&D: defining critical activities
Public/Private partnerships
M&A: the modern industry landscape
Harnessing innovation: enabling the entrepreneur
New paradigms for CRO collaboration
Day 1 Stream 2 Screening & Assays: Enabling Technologies
RNAi screening
Integrated lead discovery
Phenotypic screening
FBS-by-biochemical assays
Embryonic stem cell technologies
Assays for anti-viral research
Flow chemistry
New approaches to antibody screening
Day 1 Stream 3 Discovery Chemistry: Latest Case Studies
Structure-activity relationships
Fragment based drug discovery
Combinatorial and high-throughput chemistry
Multi-target drug discovery
Predicting solubility
Kinase data: impact on on selectivity and pharmacology profiling
Day 2 Stream 1
Innovative Drug Targets
Novel biological targets
Promising targets for neurology
Fragment-based approaches for difficult
targets
Purinome-targeted oncology libraries
Target identification in endocrinology
GPCR signalling pathways
Day 2 Stream 2
Supporting Innovation: Data & Information
Management
Using multifactorial data to improve
compound survival
Data analysis & omics data integration
Innovative compound bank programs
Sharing & consolidating information
Managing complex discovery portfolios
Day 2 Stream 3
Drug Design: Novel Approaches
Optimising allosteric kinase inhibitors
Structure based drug design
Anti-target modelling in early drug
discovery
Protein-ligand interactions: a new
theory of binding
In silico profiling of compounds
Oxford Global Conferences Are Proud To Present... The 14
th Annual Drug Discovery Leaders Summit, taking place on 10 & 11 June in Geneva. The
summit is made up of two co-located events: Innovation Driven Discovery and Discovery Chemistry & Drug Design.
The drug discovery industry faces a decade of monumental change – stem cell research, generic threat, big data challenges, PHC strategies and the growing focus on biologics all threaten to change the face of the global market. This long-established summit will explore the critical opportunities in drug discovery today, while updating key decision makers on the latest technological breakthroughs.
The Innovation Driven Discovery congress explores new approaches to screening, assay development and target identification, while experts describe the data integration technologies capable of supporting this innovation. Our esteemed speaker panel will also discuss their strategies for harnessing external innovation and building effective collaborative working methods.
The Discovery Chemistry & Drug Design congress features presentations on lead optimisation, structure-activity relationships and multi-target drug discovery. Our internationally renowned speakers will also discuss the latest developments in drug design, including anti-target modelling, new theories of protein-ligand binding and the impact of kinase data on selectivity profiling. The event will be co-located with our 5
th Annual Drug Development Congress; a high-level meeting
for those working at the forefront of research, development and translational medicine.
www.pharmaresearch-series.com
2013 Speakers
Robert Hayes Janssen
Lorenz Mayr AstraZeneca
Vic Myer Novartis
Networking And Business Meeting Opportunities Meet face-to-face with leading solution providers and senior-level industry peers through a series of formal and informal networking opportunities. Categories of solution provider include:
Drug Discovery Drug Design Medicinal Chemistry
Exploratory Medicine Target Discovery Target Validation
Screening Assay Development Lead Optimisation
Lead Generation Cell-Based Assays Data Mining
Computational Chemistry Library Design Discovery Services
Selectivity Profiling Structural Biology PK/PD Evaluation
Who You Will Meet 250 senior attendees from leading pharmaceutical, biopharmaceutical, biotechnology, diagnostics, CRO, solution provider and academic organisations. Meet Senior VPs, Directors & Managers with the following job titles:
Confirmed Speakers:
Paul Germann, Vice President New Frontier Science Europe, Takeda Robert Hayes, Vice President and Venture Leader, Centyrex Venture, Janssen R&D Emilio Diez Monedero, VP MDR & Director Basic Research Centre GSK William Strohl, VP, Biologics Research, Johnson & Johnson Lorenz Mayr, Vice President & Global Head, Reagents & Assay Development, AstraZeneca Michael Braxenthaler, President, Pistoia Alliance William Pennie, Executive Director of Compound Safety Prediction, Pfizer Vic Myer, Executive Director, Developmental and Molecular Pathways, Novartis Peter Hamley, Global Head Parallel Synthesis & Natural Products, Sanofi Aventis Campbell Wilson, Executive Business Development Director, Science & Technology Licensing, AstraZeneca Uwe Huedepohl, Vice President, R&D Project, Portfolio and Science Submission Management, MedImmune Alastair Lawson, Senior Director of Structural Biology, UCB Trevor Howe, Scientific Director and Janssen Fellow Guido Koch, Director in Global Discovery Chemistry, Novartis Ulrich Betz, Director, Department Head Innovation & Entrepreneurship Incubator, Merck Serono Andreas Marzinzik, Director, Exploratory Medicinal Chemistry, Novartis Björn Peters, Director Business Development, Shire Marius Hoener, Senior Principal Scientist, Drug Discovery Project Team Leader, Vice Director, Roche Francoise Bono, Research Director, Sanofi Henning Nielsen, Director, Novo Nordisk Sergio Cantoreggi, CSO & Global Head of R&D, Helsinn Group Tina Flatau, VP Alliances and Project Management, Prosensa David Elder, Director Scinovo, GSK R&D Daniel Baeschlin, Director Compound Management And Engineering, Novartis Institutes of BioMedical Research Andrew Leach, Director of Computational Chemistry Europe, GSK Ton Rijnders, Scientific Director, TI Pharma Karl-Heinz Baringhaus, Head of Structure, Design & Informatics, Sanofi Aventis Francisca Zanoguera, Former Head of Discovery Bioinformatics Geneva, Merck Serono Matthias Frech, Head of Molecular Interactions & Biophysics, Merck Philippe Couttet, Head Pathway Integration, Discovery and Investigative Safety, Novartis José Duca, Head, Computer-Aided Drug Discovery, Novartis Pascal Furet, Research Director, Novartis Ulrich Schopfer, Director, Integrated Lead Discovery Head, Novartis Jens Pohlmann, Head of Chemistry, Basilea Rainer E. Martin, Principal Scientist, F. Hoffmann-La Roche, Basel Johannes Grosse, Head of Discovery Biology, Takeda Wojtek Auerbach, Senior Director, Embryonic Stem Cell Technologies, Regeneron Ali Jazayeri, Head of Protein Engineering, Heptares Adrian Gill, Head of Medicinal Chemistry , CVGI, AstraZeneca Tomas Mow, Head of Department Exploratory Toxicology, H. Lundbeck A/S Ivan Efremov, Senior Principal Scientist, Pfizer Huw Rees, Senior Principal Scientist, Pfizer Julian Woelcke, Associate Director Expertise Platform Proteases, Novartis Bharat Lagu, Associate Director, Novartis Richard Morphy, Senior Research Advisor, Lilly Atli Thorarensen, Associate Research Fellow, Pfizer Eduard Felder, Director, Head of Chemical Core Technologies Dept, Nerviano Medical Sciences Patrick Jimonet, Discovery Sourcing And Leader Global Chemical Library Team, Sanofi Ian Wall, Computational Chemist, GSK Prakash Purohit, Associate Director, Scientific Affairs, Ipsen Rod Hubbard, Professor, York and Senior Fellow, Vernalis Xavier Leroy, Associate Director, Project Leader, Actelion Sjoerd Wadman, VP R&D, Lanthio Pharma Christoph Wiessner, Head of Discovery, Asceneuron Alexander Schuhmacher, Professor, School of Applied Chemistry, Reutlingen University Axel Vater, VP Drug Discovery, Noxxon Matthew Gardener, Senior Scientist, MedImmune
Day 1 – Monday 10th June
07.30 – 08.20 Registration
08.20 – 08.25 Oxford Global Welcome Address
08.25 – 08.30 Stream Chair Welcome Address
08.30 – 09.00 Keynote Presentation Collaborative Models – Different Approaches To Improve Innovation Productivity The global healthcare industry is undergoing substantial changes and adaptations to the constant decline of approved new medical entities. This decrease in internal research productivity is resulting in a major decline of patent protected sales (patent cliff) of most of the pharmaceutical companies.
Three major global adaptive trends as driving forces to cope with these challenges are evident: 1. Cut backs of internal research and development jobs in the western hemisphere 2. Follow the market growth potential of Asia by building up internal or external research and development capabilities there; 3. And finally “early innovation hunting” with an increased focus on identifying and investing in very early innovation sources within academia and small start up companies.
Paul Germann, Vice President New Frontier Science Europe, Takeda
Innovation Driven Discovery Congress Discovery Chemistry & Drug Design Congress
R&D Models For The Future Screening & Assays: Enabling Technologies Discovery Chemistry: Latest Case Studies
Stream Chair: Manfred Horst, Director Business Development, European External Scientific Affairs, Merck
Stream Chair: Henrik Konarkowski, CEO, TeaRx Stream Chair: Alex Kiselyov, President, ChemDiv
09.00 – 09.30 Stream Keynote Presentation Innovation in Drug Discovery Enabling the entrepreneur
Open source approaches
New ways of academia-industry collaboration
Leveraging the global brain pool
Ulrich Betz, Director, Department Head Innovation & Entrepreneurship Incubator, Merck Serono
Stream Keynote Presentation Integrated Lead Discovery To Tackle Difficult & Unprecedented Targets Overview of currently available lead discovery
technologies
Limitations of existing lead discovery technologies
Case studies from target-based lead discovery
Case studies from phenotypic lead discovery
Integration of lead discovery strategies
Summary and outlook
Lorenz Mayr, Vice President & Global Head, Reagents & Assay Development, AstraZeneca
Stream Keynote Presentation Discovery Research – Title to be confirmed Emilio Diez Monedero, VP MDR & Director Basic Research Centre GSK
09.30 – 10.00 Solving the Informatics Challenges in Collaborative Network Research As discovery organizations move rapidly towards a collaborative network model for research, research IT organizations are presented with significant challenges in supporting their scientists and the external partners. We will present software solutions that can help solve the problems of tech transfer and collaborative data exchange and present case studies on the use of these solutions from both the pharma/biotech and CRO point of view.
Robert Brown, Senior Director Life Sciences Research, Accelrys Inc
Solution Provider Presentation
Spinning Fragments Into Lead Molecules: A New Impulse In Fragment Based Drug Discovery ZoBio has integrated advanced & proprietary NMR
techniques into its drug discovery pipeline that yield unique synergies when combined with its other capabilities including X-ray crystallography.
ZoBio has successfully applied its technologies to more than 60 different targets including protein protein interactions, epigenetics targets and membrane protein including GPCRs to yield tractable, validated hits and leads.
This talk will describe ZoBio’s technologies and provide real life examples of how they have been used to provide our customers with ideal starting points for even the most challenging targets.
Gregg Siegal, CSO, ZoBio BV
10.00 – 11.00 Morning Refreshments One To One Meetings X 3 Exhibition & Poster Presentation Session
Day 1 – Monday 10th June
11.00 – 11.30 Open Innovation In Janssen Pharma The vision of the future landscape of healthcare in J&J J
Janssen Innovation Centre’s, the raison d’être
Effectively building and integrating public-private ventures (such as IMI programmes) into drug discovery efforts
Case studies on how to manage IP in PPP’s
Lessons learned
Trevor Howe, Scientific Director and Janssen Fellow
RNAi Screening: Go Big or Go Home The advent of sequencing technologies coupled to loss of function assessment is theoretically a powerful combination when directed towards target discovery for eventual pharmacological intervention. Yet, the promise of myriad validated targets arising from deep genomic and transcriptomic understanding of cellular systems interrogated by systematic RNAi assessment remains unrealized…
Vic Myer, Executive Director, Developmental and Molecular Pathways, Novartis
Centyrins, A New Biologics Platform For J&J Efficient production of multi-specific molecules that engage
more than one target at a time
Local delivery options such as pulmonary or nasal to CNS delivery
The attachment of cytotoxic drugs or attachment to nanoparticles for targeting applications
Robert Hayes, Vice President and Venture Leader Centyrex Venture, Janssen R&D
11.30 – 12.00 Solution Provider Presentation
Solution Provider Presentation
Solution Provider Presentation
For sponsorship opportunities please contact [email protected]
12.00 – 12.30 Innovation In Biopharma: Ipsen's Approach Overview of drug discovery innovation models in Biopharma
industry
Changing landscape in the industry
Ipsen's approach to innovation
Collaborative model - keys to success
Prakash Purohit, Associate Director, Scientific Affairs, Ipsen
Creative Collaboration Models – The Challenges For Deal-Making The drive to access innovation has generated new
creative collaboration models
These creative models require creative agreements to support them
What challenges do these agreements present and how do we address them?
Campbell Wilson, Executive Business Development Director, Science & Technology Licensing, AstraZeneca
Allosteric Interactions: Mechanism Of Actions And Consequent Biological Effects
Francoise Bono, Research Director, Sanofi
12.30 – 13.00 Mergers & Acquisitions – Title to be confirmed Björn Peters, Director Business Development, Shire
Integrated Lead Discovery – Innovation beyond Technology Drivers of change in Lead Discovery
Innovation in technology and collaborative models
The Integrated Lead Discovery strategy applied
Ulrich Schopfer, Director, Integrated Lead Discovery Head, Novartis
The Importance Of Physical Properties (Particularly Solubility) In Decreasing Drug Attrition Reasons for Attrition
Critical Role of Solubility in PK
Impact of Combinatorial and High Throughput Chemistry
Evolution of Physicochemical Properties of Marketed Drugs
Importance of lipophilicity (logP) and MP in solubility
Strategies to improve ADMET properties (including solubility)
Predicting solubility (SFI)
Impact on Various Developability Criteria
David Elder, Director Scinovo, GSK R&D
13.00 – 14.00 Lunch – Helvetia A & B & Foyer One to One Meetings x 2
Day 1 – Monday 10th June
14.00 – 14.30 Collaboration: What Is It Going To Do For Us?
Biopharma and the importance of collaborations
Collaboration options and styles
Achieving win-win
Tina Flatau, VP Alliances and Project Management , Prosensa
Flow Chemistry - An Enabling Tool in Drug Discovery Discovery chemistry
Enhanced process window
Automation in flow
Rainer E. Martin, Principal Scientist, F. Hoffmann-La Roche, Basel
Antibodies As Tools In Small Molecule Drug Discovery Antibodies have successfully addressed modulation of
protein-protein interactions in the clinic, and are set to enable the discovery of small molecules, which have similar biological activities. Such small molecules may be considered as ‘chemosuperiors’, as they can be expected to follow on from pioneering therapeutic antibodies, but display improved drug characteristics.
Antibodies have already proved to be of significant value as chaperones in crystallography.
Antibodies are now being used to define specific conformations of proteins, providing new and previously unexpected opportunities for intervention with small molecules.
Small molecule fragment screening against antibody-constrained targets offers the prospect of discovering new chemical entities, which would otherwise be unable to gain a foothold on proteins. The approach is particularly well suited to the discovery of small molecules which modulate protein-protein interactions through binding at allosteric sites.
Alastair Lawson, Senior Director of Structural Biology, UCB
14.30 – 15.00 Library-Scale Gene-Expression Profiling and Digital Open Innovation Match diseases with drugs through the transitive property of
common gene-expression changes
Realized through library-scale gene-expression profiling technology, online database of small-molecule gene-expression profiles, and simple self-service search engine
Digital open-innovation medium creates self-selected partnerships between domain-expert biologists and the owners of proprietary chemical matter
Justin Lamb, President and CEO, Genometry
Solution Provider Presentation
Reserved: Axiogenesis
Solution Provider Presentation
For sponsorship opportunities please contact [email protected]
Day 1 – Monday 10th June
15.00 – 15.30
Public/Private Partnerships: A Potential Solution For The Modern Pharmaceutical Industry Public-private partnerships in drug discovery in the
Netherlands
Critical success factors
The European perspective
The European Lead Factory
Ton Rijnders, Scientific Director, TI Pharma
Panel Discussion: Innovations In Screening Assessing different screening approaches
Continuous hit-finding
Utilising bioinformatics tools
Advances in biologics screening
Antibody tools for screening
(Chair) Eduard Felder, Director, Head of Chemical Core Technologies Dept, Nerviano Medical Sciences Vic Myer, Executive Director, Developmental and Molecular Pathways, Novartis Alastair Lawson, Senior Director of Structural Biology, UCB
New Models For Lead Generation The risk-sharing approach for accessing innovative
chemical space
Exposing Sanofi's chemical space to new biological innovation
New models to fully exploit Sanofi's natural product universe
Peter Hamley, Global Head Parallel Synthesis & Natural Products, Sanofi Aventis
15.30 – 16.00 Virtual R&D: The Helsinn Success Story The Helsinn R&D structure and its performance
Definition of core and critical activities
CRO selection and monitoring: focus on quality and relationships
The Aloxi success story
Join forces with other mid-pharma companies
The "human factor"
Sergio Cantoreggi, CSO & Global Head of R&D, Helsinn Group
The Spiegelmer® Therapeutics Discovery Platform: From Evolution In Vitro To Efficacy In Vivo Spiegelmers are plasma-stable oligonucleotides that are
generated by in vitro evolution from random DNA or RNA libraries. They bind and neutralize a target of interest.
Similar to antibodies, Spiegelmers can inhibit large-surface interactions between proteins where small molecules often fail.
In contrast to antibodies, Spiegelmers are produced by a chemical process and stimulation of the immune system or generation of anti-drug antibodies have not been observed.
Efficacy in vivo has been shown for several Spiegelmers. Three candidates are currently in four international Phase IIa studies.
Axel Vater, VP Drug Discovery, Noxxon
Increasing Effectiveness Of Early Drug Discovery Projects Teams Integrated Lead Finding (ILF) in early drug discovery is a coordinated approach involving different disciplines. A diagnostic exercise to understand the critical factors will be presented. Key areas enabling successful lead finding will be discussed. A particular focus of the presentation will cover leadership challenges faced by R&D teams. The distributed leadership concept will be introduced and suggestions for drug discovery teams will be presented.
Guido Koch, Director in Global Discovery Chemistry, Novartis
16.00 – 16.40 Afternoon Refreshments One To One Meetings X 2 Exhibition & Poster Presentation Session
16.40 – 17.10
Is There A New Business Model For Pharma Innovation? Open innovation in the pharmaceutical industry
Examples for inside-out and outside-in processes
R&D strategies of pharmaceutical companies
New business models in R&D offer new opportunities
Alexander Schuhmacher, Professor, School of Applied Chemistry, Reutlingen University
Screening & Assays Concept of continuous hit finding
FBS-by-biochemical assays
Fluorescence lifetime as powerful new readout for lead discovery
Julian Woelcke, Associate Director Expertise Platform Proteases, Novartis
Enhancement Of Chemical Matter For Lead Finding Through Innovative Business Models Lessons learned from failure in development at Sanofi
and evolving discovery portfolio highlight the need to access improved chemicals and novel chemical space
Chemical matter improvement for Lead finding through innovative business models: risk-shared partnerships and other novel models to replace traditionnal buy-and-sell, or explore new opportunities; examples of implemented deals
Patrick Jimonet, Discovery Sourcing And Leader Global Chemical Library Team, Sanofi
Day 1 – Monday 10th June
17.10 – 17.40 Redefining ‘CRO’ To Mean ‘Creative Research
Opportunities’ Big Pharma’s evolving drug discovery paradigms in working
with CROs: collaboration is a two-way street
Defining metrics and successes with new paradigms
Case study-lessons learned
Bharat Lagu, Associate Director, Novartis
Gene Targeting in Embryonic Stem Cells as a Tool for New Targets Discovery, Therapeutic Antibody Production and Drug Validation Understanding the function of each gene and expression
pattern
Development of mice producing fully human monoclonal antibody
Delivering unprecedented speed and capacity for the validation of therapeutic targets in humanized mice
Wojtek Auerbach, Senior Director, Embryonic Stem Cell Technologies, Regeneron
Discovery Chemistry Case Studies: Structure Activity Relationships
Drug Residence Time
Matthias Frech, Head of Molecular Interactions & Biophysics, Merck
17.40 – 18.10 Opportunities And Challenges In Drug Discovery For Alzheimer's Disease Why is Alzheimer's Disease emerging as one of the largest
healthcare problems worldwide
What is the unmet medical need in AD
What has worked, what has failed and why, and what is currently explored clinically
What are the most promising and innovative new treatment strategies and targets in AD drug discovery
Christoph Wiessner, Head of Discovery, Asceneuron
Exploratory Toxicology Fully Integrated Into Drug Discovery In an effort to reduce toxicity-related attrition, different strategies have been implemented throughout the pharmaceutical industry. When a development candidate is selected the properties of the molecule are fixed, including those causing toxicity. Therefore, only during the drug discovery phase one has the chance to modify these properties. At Lundbeck, exploratory toxicology research has been fully integrated into the drug discovery process. The aim is to not only provide timely go/no go decisions (“fail early”), but rather also provide a direction to the drug discovery teams (“show what will not fail”), by steering away from potential liabilities during drug discovery. Examples of compound testing paradigms using early in vitro, ex vivo and in vivo assays and models to assess safety risks will be presented. Instead of testing “everything early” we aim to test “the right things at the right time” by focusing on toxicities and adverse events which occur frequently and/or have high impact during the development of novel drug candidates. Furthermore considerations for the choice of assays, including predictivity, throughput, and turn-around time will be discussed.
Tomas Mow, Head of Department Exploratory Toxicology, H. Lundbeck A/S
ATP Mediated Kinome Selectivity Impact of using kinase data generated under Km condition
for interpretation of selectivity and pharmacology
Alternative discovery paradigm for kinase drug discovery projects
Examples for several kinase project will be provided
Expansion of this to different classes of kinase inhibitors (eg. type 2) will be discussed.
Atli Thorarensen , Associate Research Fellow, Pfizer
18.10 – 18.40 Polypharmacology Presents Opportunities For Open Innovation Richard Morphy, Senior Research Advisor, Eli Lilly
Screening Of Biologics During The Lead Identification Phase: New Assay Technologies And Functional Approaches Used Moving beyond traditional antibody screening approaches
Targeting complex membrane proteins
Functional screening of biologics
Matthew Gardener, Senior Scientist, MedImmune
Challenges For Fragment-Based Drug Discovery Fragment-based methods are now successfully delivering clinical candidates, but challenges remain. For conventional targets these are mainly organisational; for non-conventional targets (such as protein-protein) there are additional technical challenges which we are only beginning to understand.
Rod Hubbard, Professor, York and Senior Fellow, Vernalis
18.40 Networking Drinks
Day 2 – Tuesday 11th June
Stream Chair
08.30 – 09.00 Keynote Presentation Using Multifactorial Data To Improve Compound Survival In Drug Discovery The incorporation of predictive toxicology approaches in early preclinical drug development will be important for reducing the attrition rate within the industry. To identify potential toxic compounds and guide medicinal chemistry efforts, targeted in vitro assays have been integrated with structure activity-relationship rules and physicochemical properties to predict in vivo effects…
William Pennie, Executive Director of Compound Safety Prediction, Pfizer
Innovation Driven Discovery Congress Discovery Chemistry & Drug Design Congress
Innovative Drug Targets Supporting Innovation: Data Integration, Analysis &
Management
Drug Design: Novel Approaches
Stream Chair: Oliver Lehner, VP Sales Europe & APAC, Definiens AG
Stream Chair: DDS
09.00 – 09.30 Stream Keynote Presentation Targets for Biologics – Choice Of Targets And Biological Approach There is significant competition on the “hot” targets, which
will result in a sorting out of those that are not “first-in-class” or “best-in-class”
New targets will create innovation in the antibody field
Novel targets may require novel approaches including use of alternative scaffolds or peptides
William Strohl, VP, Biologics Research, Johnson & Johnson
Stream Keynote Presentation The Role of Pre-Competitive Collaboration in the Search for Innovation Models in Biomedical R&D Does pre-competitive collaboration deliver true innovation
or just efficiency gains?
Hurdles and opportunities for pre-competitive collaboration
The Pistoia Alliance in the pre-competitive collaboration landscape
Michael Braxenthaler, President, Pistoia Alliance
Stream Keynote Presentation Anti-Target Modelling In Early Drug Discovery Modern drug discovery aims to achieve development compounds with a clean profile. Any effects on anti-targets (e.g. hERG, CYP2D6, CYP2C9, CYP3A4, a1a, ...) or potential toxic liabilities (e.g. Phospholipidosis, CYP induction, phototoxicity) should be avoided. Computational chemistry enables early assessment of anti-target effects of compounds as well as design principles to get rid of these activities. This presentation captures several techniques to build and validate anti-target models as well as its application in hit to lead and lead optimization. The emerging field of polypharmacology and in silico profiling of compounds will be also addressed.
Karl-Heinz Baringhaus, Head of Structure, Design & Informatics, Sanofi Aventi
09.30 – 10.00 Solution Provider Presentation
Solution Provider Presentation
CONFIRMED: Thomson Reuters
Solution Provider Presentation
For sponsorship opportunities please contact [email protected]
10.00 – 10.30 Solution Provider Presentation
For sponsorship opportunities please contact [email protected]
Solution Provider Presentation
RESERVED: Certara
Solution Provider Presentation
For sponsorship opportunities please contact [email protected]
10.30 – 12.10 Morning Refreshments One To One Meetings X 5 Exhibition & Poster Presentation Session
12.10 – 13.10 Lunch One To One Meetings x 2
Day 2 – Tuesday 11th June
13.10 – 13.40
Target Identification In Endocrinology: Case Studies In Favour Of Private-Public Collaborations In addition to established members of endocrine systems
recently discovered factors are the ‘hot spots’ for pharmacological intervention
Enteroendocrine hormones are the main signals of the gut-brain axis which is responsible for the efficacy of bariatric surgery
The recent discovery of novel players in the complex response pattern of enteroendocrine hormones to fasting and feeding opens new opportunities for drug discovery.
Johannes Grosse, Head of Discovery Biology, Takeda
Omics Data Integration Drug-induced heart liabilities is a safety concern in drug
development
We have studied the Doxorubicin-induced cardiotoxicity mechanism at the transcriptomic (mRNA and microRNA) level in rodents and anchored these data to histopathology observation and clinical chemistry endpoints.
We have built up a transcriptomic (mRNA and microRNA) heart Atlas of 8 heart structures across species and identified heart structure specific gene signatures.
Philippe Couttet, Head Pathway Integration, Discovery and Investigative Safety, Novartis
Identification And Optimization Of Allosteric Kinase Inhibitors How to find and characterize allosteric kinase inhibitors?
Optimization of potency, selectivity, clearance, and PK
In vivo proof of concept for the allosteric paradigm on IGF1R
Andreas Marzinzik, Director, Exploratory Medicinal Chemistry, Novartis
13.40 – 14.10
Targeting The Nav1.7 Sodium Channel Mechanistic studies exploring the role of NaV1.7 in rats
and mice
Being more clinical about experimental design; addressing bias in preclinical studies
Future directions; re-evaluating the role of spinal dorsal horn neurones in models of nerve injury
Huw Rees, Senior Principal Scientist, Pfizer
Enabling Drug Discovery Through Innovative Compound Sample & Data Workflows The compound management groups of the Novartis Institutes of BioMedical Research (NIBR) are challenged by increasingly changing requirements: drug discovery project teams operate globally across the eight research sites, employ an increasing number of technologies for lead finding & lead optimisation and continue to grow the number of requested compound samples. NIBR has therefore initiated a major program called “Novartis compound bank” to transform its compound sample handling infrastructure into an adaptable, modular framework of hardware and software systems enabling not only reliable and efficient sample handling, but also flexibility in process adaptation. The presentation will detail not only NIBR’s vision for this modern infrastructure, but also the actual benefits for the drug discovery processes of the first part of the implementation.
Daniel Baeschlin, Director Compound Management And Engineering, Novartis Institutes of BioMedical Research
Reconsidering Protein-Ligand Interactions And Drug Design Through Disruptive Thinking Protein-Ligand Interactions reassessed via innovative ways
to understand how proteins function
A whole new theory of binding arising
Dynamic imprints of proteins can gate selectivity and specificity
José Duca, Head, Computer-Aided Drug Discovery, Novartis
Day 2 – Tuesday 11th June
14.10 – 14.40
Discovery And Characterization Of TAAR1 Agonists, Modulators Of Dopaminergic And Serotonergic Neurotransmission With Therapeutic Potential In Neuropsychiatric Disorders The trace amine-associated receptor 1 (TAAR1) is a G
protein-coupled receptor activated by trace amines like p-tyramine and beta-phenylethylamine, endogenous compounds with structural similarity to biogenic amines.
TAAR1 agonists were developed, characterized and, together with TAAR1 transgenic animals, used to evaluate TAAR1 as a potential drug target for neuropsychiatric disorders.
TAAR1 partial agonists are proposed to be superior to existing atypical antipsychotic drugs based on preclinical studies by displaying antipsychotic efficacy with the benefit of improved cognition and mood as well as with a reduced side effect profile (e.g., no sedation, no weight gain, no extrapyramidal symptoms).
Marius Hoener, Senior Principal Scientist, Drug Discovery Project Team Leader, Vice Director, Roche
IMI OpenPHACTS Initiative Andrew Leach, Director of Computational Chemistry Europe, GSK
Lead Optimisation Case Histories In The Diabetes And Obesity Area
Adrian Gill, Head of Medicinal Chemistry , CVGI, AstraZeneca
14.40 – 15.10 Fragments And Enablement Of Tough Targets – Beta-Secretase As The Case Study The talk will highlight application of fragment-based approaches to accelerate identification and optimization of chemical matter for a difficult target – beta-secretase. Diversity-based and knowledge-based approaches will be discussed as alternative and complementary hit ID strategies together with use of fragment-derived information to accelerate progression of a more advanced series. Multidisciplinary approach was the key to rational decision making in the hit optimization process and will be a focal point of the talk.
Ivan Efremov, Senior Principal Scientist, Pfizer
Innovation Is Fostered By Information And Knowledge Trends and strategies in information management
Henning Nielsen, Director, Novo Nordisk
Optimization of an Anti-Cancer Lead Novel microtubule destabilizers with a unique mode of
action were identified
Low solubility presented a hurdle for further development
Systematic evaluation of prodrugs provided a compound for clinical development
Jens Pohlmann, Head of Chemistry, Basilea
15.10 – 15.30 Afternoon Refreshments
15.30 – 16.00 Stabilised Receptor (StaR) Technology Enables Structure Based Drug Design For GPCRs Introduction to Heptares
Introduction to StaR technology
Utility of StaRs for SBDD
Ali Jazayeri, Head of Protein Engineering, Heptares
Successful Management Of MedImmune’s Complex And Rich Discovery Portfolio In the talk I will introduce the complexity (size and
diversity) of our MedImmune Research portfolio
Explain the way how we manage it
And show the linkage between the way it is managed to the success in delivery
Uwe Huedepohl, Vice President, R&D Project, Portfolio and Science Submission Management, MedImmune
The Design Of MDM2-p53 Antagonists In The Protein-Protein Interaction (PPI) Area Generic approaches in the design of PPI inhibitors
Pocket adapted approach: the generation of new p53-MDM2 inhibitor scaffolds by pure structure-based design
Optimization towards in vivo efficacious compounds
Pascal Furet, Research Director, Novartis
Day 2 – Tuesday 11th June
16.00 – 16.30 Purinome Targeted Libraries In Oncology Research The generation of novel chemotypes for oncology projects
expands from a canonical design of kinase-targeted compound libraries to a broader interpretation of purinome-targeted libraries (PTL).
Screening of structurally diverse ATP-binding targets calls for compound libraries covering multiple design elements, which may include phosphate surrogate moieties in ATPase inhibitors or far reaching lipophilic residues stabilizing inactive kinase conformations.
We compared overall hit rates of PTL with a simultaneously tested unbiased collection of 200,000 compounds and confirmed that a multidisciplinary support of library design translates into significantly more effective targeted libraries.
The performance analysis of various chemotypes on a panel of ATP-binding targets facilitates the exploitation of drug discovery synergies across the whole purinome
Eduard Felder, Director, Head of Chemical Core Technologies Dept., Nerviano Medical Sciences
Computational Approaches in Fragment Based Drug Discovery Development and use of computational tools for data
management and analysis, structure-based design and ligand-based design
Examples of application to drug discovery programmes
Discussion of gaps in current capabilities and efforts to address the gaps
Ian Wall, Computational Chemist, GSK
Lanthipeptides : New Therapeutic Applications for Nature’s own Stabilised Peptides Introduction to Lanthipeptides
Harnessing natural biosynthetic systems for therapeutic uses
Case study : Lantipeptides as specific GPCR agonists
Sjoerd Wadman, VP R&D, Lanthio Pharma
16.30 – 17.00 Innovation In GPCR Research And Signalling Pathways Xavier Leroy, Associate Director, Project Leader, Actelion
How Data Analysis Can Help Drug Discovery – Title to be confirmed Francisca Zanoguera, Former Head of Discovery Bioinformatics Geneva, Merck Serono
Delegates are welcome to attend the co-located presentation.
17.00 End of Conference