Running Parallel with 2 events, 1 Price 5th Annual Optimise your therapeutic programmes with the latest advances and cutting edge developments across peptide research, discovery, development, clinical, manufacturing and delivery stages 18 - 19 November 2014 Maritim proArte Hotel, Berlin, Germany £499 Academic Price 50% Discount for Start-Ups & Small Businesses* KEY SPEAKERS INCLUDE: Lars Fogh Iversen, Executive Vice President, Novo Nordisk, Denmark Horst Kessler, Emeritus of Excellence, Institute for Advanced Study at the Technische Universität München, Germany Angelika Fretzen, Vice President of Pharmaceutical Chemistry & Development, Ironwood Pharmaceuticals, USA Matthias Urmann, Associate Vice President, Research & Translational Medicine, Insulin & Peptides, R&D, Diabetes Division, Sanofi-Aventis Deutschland GmbH, Germany Lutz Jermutus, Senior Director, R&D & Product Development Team Leader, Cardiovascular & Metabolic Diseases iMED, MedImmune Ltd, UK Dinesh Patel, President & CEO, Protagonist Therapeutics, USA David Craik, Group Leader, Institute for Molecular Bioscience, The University of Queensland, Australia Michael Shapiro, Director, Analytical Research Technologies, Pfizer Pharmaceuticals, USA EVENT SPONSORS www.informa-ls.com/peptides Advance Your Peptide Therapeutics Towards Commercial Success Dear Colleague, Companies are investing huge amounts of resources into developing peptide-based therapeutics, and the global market is expected to reach $25.5 billion by 2018. With significant advances in this area of biologics, EuroPEPTIDES has been specifically designed to explore the latest advances in peptide science, and the most successful and effective techniques for peptide development. Working closely with our event Advisory Board, we have developed a combination of 2 tracks, 30+ industry speakers, 3 exciting workshops and 10+ hours of exclusive networking activities, to bring together leading decision - makers across peptide research to hear the latest updates from pre-clinical and clinical programmes and drive improvements in R&D, formulation, half-life extension, manufacturing and analytical strategy. In addition, for this year we’ve introduced a brand new focused conference stream on early stage research and discovery, to help you maximise learning opportunities and explore cutting edge peptide therapeutic research. I look forward to seeing you in Berlin. Good conference that addresses current needs and challenges Amy Fry Conference Producer Biopharm Conference Series Informa Life Sciences NEW FOR 2014 Janssen Pharmaceuticals STREAM 1: Research and Discovery • 15+ focused talks • Gain insight on cutting edge peptide research • Uncover the current developments in macrocyclic and constrained peptides • Identify promising novel targets and indications • Advance your peptide design programme STREAM 2: Development and Manufacturing •E nhance your understanding of new formulation strategies •O ptimise your manufacturing and analytical strategy •A ssess the advantages of microwave assisted solid phase peptide synthesis •E xplore alternative methods to improve the half-life capabilities Case studies from industry experts including Novo Nordisk, Ipsen, Bicycle Therapeutics, Ironwood Pharmaceuticals, Janssen, Novartis, Pfizer, Protagonist Therapeutics, MedImmune, Bachem, Polypeptide, Nexigen, Roche, University of Queensland + many more… www.informa-ls.com/peptides Agenda Day One Click on the presentation for more information Tuesday 18th November 2014 OPENING PLENARY ADDRESS 08:00 Registration and Morning Coffee 08:50 Opening Remarks from Chairperson 09:00 KEYNOTE: GLP-1 Peptide Engineering Dr Lars Fogh Iversen, Executive Vice President, Novo Nordisk, Denmark 09:40 KEYNOTE: Oral Bioavailability of Peptides Professor Horst Kessler, Emeritus of Excellence, Institute for Advanced Study at the Technische Universität München, Germany 10:20 Panel Discussion: Emerging Trends in Peptide Development 11:00 Morning Coffee and Exhibition/Poster Viewing Time STREAM 1: Research & Discovery CONSTRAINED AND MACROCYCLIC PEPTIDES: ARE THEY WORTH THE FUSS? 11:30Development of Bicyclic Peptides to Target Protein- Protein Interactions r Dan Teufel, D Head of Chemistry, Bicycle Therapeutics, UK STREAM 2: Development and Manufacturing ANALYTICAL METHODS FOR PEPTIDE CHARACTERISATION 11:30 BYRO5 Peptides – Analytical Tools Dr Michael Shapiro, Director, Analytical Research Technologies, Pfizer Pharmaceuticals, USA 12:05 Spotlight Presentation 12:05 Disulfide-Rich Peptide Cyclisation Professor David Craik, Group Leader, Institute for Molecular Bioscience, University of Queensland, Australia This presentation will be hosted by a leading company operating in the field of peptides. Please contact [email protected] for more details +44 (0)207 017 5011 12:40 Lunch and Exhibition/Poster Viewing Time 12:40 Lunch and Exhibition/Poster Viewing Time NON-INVASIVE METHODS FOR DELIVERY AND FORMULATION 14:00Panel Discussion: Comparing the Advantages Between 14:00Alternative Peptide Delivery Technologies: A Focus on r Waleed Danho, D Former, Distinguished Research Leader, Roche, USA r Andy Lewis, Director, Novel Delivery Technologies D CMC & Engineering-Peptides – Technical Operations, Ipsen, France rofessor Horst Kessler, Emeritus of Excellence, P Institute for Advanced Study at the Technische Universität München, Germany r Joël Richard, Senior Vice President, D Peptides - CMC & Engineering – Technical Operations, Ipsen, France rofessor David Craik, P Group Leader, Institute for Molecular Bioscience, University of Queensland, Germany 14:35Oil-Based Formulations for Oral Delivery of Peptides Dr Roger New, Co-Founder & Director, Proxima Concepts Ltd, UK the Oral Route Linear and Cyclic Peptides for Intracellular Delivery CLINICAL AND PRECLINICAL UPDATES 14:35Oxytocin: New Interests in a Rather Old Molecule Dr Konrad Bleicher, Medicinal Chemistry, Peptide Area Head, pRED, Roche Innovation Centre Basel, F. Hoffmann-La Roche, Switzerland 15:10The Journey From De-Novo Discovery to Pre-clinical Development of IL-6 Peptide Antagonists as Novel Antiinflammatory Agents r Dinesh Patel, D President & CEO, Protagonist Therapeutics, USA 15:45Afternoon Tea with Exhibition/Poster Viewing Time 16:15Lessons from an Intranasal, Neuroprotective Peptide, NAPVSIPQ. Why Did It Fail? r Bruce Morimoto, D Executive Director, Applied Translational Medicine, Celerion, USA 15:10 Spotlight Presentation 15:45 Afternoon Tea with Exhibition/Poster Viewing Time 16:15Degradation Kinetics & Aggregation Tools: A Combinatorial Approach to Discern Real-time Formulation Stability of a Pharmaceutical Peptide that can aid Infrequent Dosing of Peptides r Lutz Jermutus, Senior Director, R&D & Product D Development Team Leader, Cardiovascular & Metabolic Diseases iMED, MedImmune Ltd, UK r Matthias Urmann, Associate Vice President, Research D & Translational Medicine, Insulin & Peptides, R&D, Diabetes Division, Sanofi-Aventis Deutschland GmbH, Germany r Oliver Demmer, D Scientist, Medicinal Chemistry, Zealand Pharma, Denmark Treatment of Functional Gastrointestinal Disorders r Angelika Fretzen, Vice President of Pharmaceutical D Chemistry & Development, Ironwood Pharmaceuticals, USA 17:25End of Conference Day One followed by Networking Drinks Reception r Adrian Podmore, D Formulation Scientist, MedImmune, UK 16:50Panel Discussion: Exploring the Advances in Technology 16:50Highlights from the Development of Linaclotide for the This presentation will be hosted by a leading company operating in the field of peptides. Please contact [email protected] for more details +44 (0)207 017 5011 17:25 End of Conference Day One followed by Networking Drinks Reception www.informa-ls.com/peptides Agenda Day Two Wednesday 19th November 2014 08:30 08:55 Registration and Morning Coffee Opening Remarks from Chairperson STREAM 1: Research & Discovery NOVEL TARGETS, INDICATIONS AND TARGET VALIDATION 09:00A Lanthipeptide Agonist of the Angiotensin II Type 2 Receptor for Treatment of Fibrosis. r Gert Moll, D CSO, Lanthio Pharma, Netherlands rofessor Dieter Willbold, Director, Institut für Physikalische P Biologie, Heinrich-Heine-Universität, Düsseldorf and Director, Institute of Complex Systems, ICS-6: Structural Biochemistry, Research Centre Jülich, Germany 10.10Engineered Affibody Molecules: Emerging Peptide Drug Candidates for Targeted Therapy r Joachim Feldwisch, D Director Preclinical Development, Affibody, Sweden 11.15Antibiofilm Peptides Against the Fungal Pathogen Candida Albicans: Mode of Action and Structure-Activity Relationship r Karin Thevissen, D Industrial Research Manager, KU Leuven, Belgium 11.50Harnessing mRNA-display for the Discovery of Macrocyclic Peptide Drugs Kristopher Josephson, Dr Director of Molecular Biology, RA Pharmaceuticals Inc, USA Expression and Bioconjugation r Lutz Jermutus, Senior Director, R&D & Product D Development Team Leader, Cardiovascular & Metabolic Diseases iMED, MedImmune Ltd, UK 09.35 Chemical Synthesis of Peptide Macrocycles Dr Thomas Meier, Vice-President Production, Bachem AG, Switzerland 10:10 Assessing the Applications of Microwave Assisted Solid Phase Peptide Synthesis r Andreas Rybka, D Head of Peptide Chemistry, Nexigen GmbH, Germany 10.45 Morning Coffee and Exhibition/Poster Viewing Time 11:15Solid-Phase Peptide Synthesis: Microwave Heating and SCREENING AND PEPTIDE LIBRARY DEVELOPMENT 09:00Therapeutic Peptides Through Synthesis, Recombinant 10.45 Morning Coffee and Exhibition/Poster Viewing Time MANUFACTURING AND PROCESS DEVELOPMENT Directed Therapy of Alzheimer’s Disease STREAM 2: Development and Manufacturing 09:35Stable D-Enantiomeric Peptides for the Aβ Oligomer Click on the presentation for more information New Reagents r Knud Jensen, D Professor of Nanobioscience, Department of Chemistry, University of Copenhagen, Denmark 11:50 Current and Future Challenges of Peptide Manufacturing Dr Jon Rasmussen, Director, Global Development, PolyPeptide, Denmark 12:25Panel Discussion: Synthetic versus Recombinant Techniques for Peptide Synthesis? 12.25 Spotlight Presentation This presentation will be hosted by a leading company operating in the field of peptides. Please contact [email protected] for more details +44 (0)207 017 5011 13:00 Lunch and Exhibition/Poster Viewing Time 13:00 Lunch and Exhibition/Poster Viewing Time BIOCONJUGATION TO IMPROVE HALF LIFE: WHAT ARE THE ALTERNATIVES TO PEGYLATION? OPTIMISING PEPTIDE DESIGN, MODE OF ACTION AND NOVEL TECHNOLOGIES 14.10Reviewing Effective Techniques for Designing Multi- 14:10 Investigating Molecular Technologies that can Extend Specific Acting Peptides Towards Infrequent Dosing r Oliver Demmer, D Scientist, Medicinal Chemistry, Zealand Pharma, Denmark Bacterial Biofilms Professor Charles Deber, Senior Scientist, Division of Molecular Structure & Function, Research Institute, Hospital for Sick Children, Toronto; and Professor, Department of Biochemistry, University of Toronto 15:50Discovery and Structure-Based Optimisation of Peptidic and 15:50PASylation: A Uniform Biosynthetic Polymer with PEG- Like Biophysical Properties for the Development of Peptides and Proteins with Enhanced Action 16.25Exploiting The Biophysical Properties Of Centyrins For Targeted Delivery Non-Peptidic Inhibitors Targeting the Adenoviral Protease r Eva Altmann, D Senior Investigator, Novartis Institute for Biomedical Research, Switzerland Vadim Dudkin, Dr Associate Director, Centyrex, Janssen R&D, USA 17:00Closing Remarks from Chairperson This presentation will be hosted by a leading company operating in the field of peptides. Please contact [email protected] for more details +44 (0)207 017 5011 15:20Afternoon Coffee and Exhibition/Poster Viewing Time 15:20Afternoon Coffee and Exhibition/Poster Viewing Time r Cyrille Gineste, D Chief Scientific Officer, Riogin Corp, USA 14.45 Spotlight Presentation 14:45 Development of Novel Peptide Antibiotics Against Peptide Half-Life r Lars Friedrich, D Scientist, XL-Protein GmbH, Germany 16:25XTEN – A Biodegradable Alternative to PEG for Half-Life Extension and Drug Delivery Volker Schellenberger, Dr President and CEO, Amunix Operating Inc., USA 17:00Closing Remarks from Chairperson 17:10End of Conference 17:10End of Conference www.informa-ls.com/peptides Pre-Conference Workshop & Seminar Monday 17th November & Tuesday 18th November 2014 PRE-CONFERENCE WORKSHOP (Y): MONDAY 17 NOVEMBER 2014 SUCCESSFUL STRATEGIES FOR OPTIMISING DESIGN AND VALIDATION OF MACROCYCLIC AND CONSTRAINED PEPTIDES Registration will be at 13:30 for a 14:00 start. The workshop will finish no later than 20:00. Workshop documents, refreshments and an evening meal will be provided. NEW FOR 2014 Reasons to attend: Delegates will be given the opportunity to enhance their understanding and explore essential considerations in developability and the R&D process for macrocyclic and constrained peptides, including design, validation and lead optimisation aspects. Key themes will include: • Reviewing the successful strategies of cyclising peptides and design considerations • Validation methods to ensure specificity and potency for desired target • Assessing the mode of action and triggering of cell functionality • Utilisation of technology to identify cyclic peptide candidates • Understanding the relationship between stability and bioavailability • Ensuring the production of stable molecules to enable nondegradation / resistance in cells Session Leaders: Professor David Craik, Group Leader, Institute for Molecular Bioscience, University of Queensland, Australia Dr Roger New, Co-Founder & Director, Proxima Concepts Ltd, UK Dr Ron Jackson, Principal Scientist, Antibody Discovery and Protein Engineering, MedImmune, UK EVENING SEMINAR (S): TUESDAY 18 NOVEMBER 2014 EXPLORING THE DEVELOPMENT OF PEPTIDES FOR DIAGNOSTIC APPLICATIONS Registration will be at 18:30 for a 18:45 start. The seminar will finish no later than 20:30. Seminar documents will be provided and an evening networking dinner will be included after the session. NEW FOR 2014 Reasons to attend: This evening seminar will give attendees the chance to discover the latest progress in this field of peptide research and enhance their understanding of the key considerations in design, target validation, and optimisation as well as potential application areas such as preclinical diagnostic imaging and biomarkers. Key themes will include: • Outlining methods for conjugation of peptides to radioactive tags • Reviewing new techniques that enable site specific modifications of peptides • Assessing which markers are used and how • Overview of the screening techniques used for detection Session Leaders: Dr Carsten Grötzinger, Group Leader, Hepatology & Gastroenterology Department, Charite Universitatsmedizin Berlin, Germany Dr Sebastian Dziadek, Development Leader R&D, PHC Assay Development, Roche Diagnostics GmbH, Germany www.informa-ls.com/peptides Post Conference Focus Day Thursday 20th November 2014 POST CONFERENCE FOCUS DAY (Z): THURSDAY 20 NOVEMBER 2014 EFFECTIVE DEVELOPMENT AND MANUFACTURING STRATEGIES FOR PEPTIDE PRODUCTION IN CONTRACTED PARTNERSHIPS Registration is at 08:30 for a 09:00 start. The session will finish no later than 15:00. Conference documents, lunch and refreshments will be provided. Reasons to attend: This Focus Day will explore the key considerations in peptide development, and important factors to take into account when selecting a business partner. The essential technical and business aspects of process and analytical development will be discussed to ensure commercial and regulatory success. New for this year, the workshop will include case studies from leading industry professionals, who will share their expertise with the delegates offering the chance for benchmarking best practices and sharing lessons learned. With plenty of opportunity for interactive and informative discussion, delegates will learn successful strategies for optimising the manufacture of peptide therapeutics. Key themes will include: • Process development: - Process development and manufacturing management - Analytical considerations • Process scaling up: - Strategy and resource optimisation - Process validation and regulatory requirements • CDMO Management: - Contract Manufacturing Management - Managing IP and tech transfer challenges • Later stage manufacturing and commercial life cycle Session Leaders: Dr Vincent Bille, Founder & Managing Director, Marble Pharma Consult SPRL, Belgium Dr Bruce Morimoto, Executive Director, Applied Translational Medicine, Celerion, USA With Thanks to the EuroPEPTIDES 2014 Advisory Board: Waleed Danho, Former, Distinguished Research Leader, Roche, USA Jesper Lau, Vice President, Diabetes Protein & Peptide Chemistry, Novo Nordisk, Denmark Volker Schellenberger, President and CEO, Amunix Operating Inc, USA Neil Thompson, Associate Director, Business Development, Europe, PolyPeptide Laboratories A/S, Denmark Matthias Urmann, Associate Vice President, Research & Translational Medicine, Insulin & Peptides, R&D, Diabetes Division, Sanofi-Aventis Deutschland GmbH, Germany Bruce Morimoto, Executive Director, Applied Translational Medicine, Celerion, USA Lutz Jermutus, Senior Director, R&D & Product Development Team Leader, Cardiovascular & Metabolic Diseases iMED, MedImmune Ltd, UK Boris Corpataux, Director of Sales, Bachem, Switzerland Present a Poster You must be booked on as a delegate to be able to present a poster. To apply, please send your abstract of 200 words or less, written in English, listing the principle author and all contact details to [email protected] • Posters submitted by academic institutions and industry will not be charged a fee • Posters submitted by service providers/vendors are welcome and will be subject to evaluation by the scientific advisory board. Upon approval a fee of £399 + 19% VAT will apply Poster application deadline: Monday 27 October 2014 www.informa-ls.com/peptides Sponsorship & Exhibition Great place to get information / networking opportunities. 7 reasons to sponsor 1. Create sales opportunities 2. Make new contacts 3. Strengthen existing relationships 4. Increase your company profile 5. Develop insight into the market 6. Position your portfolio against competitors 7. Meet an international audience Merck Millipore A place to be when you are interested to get the latest updates in the hot-topics about peptide therapeutics as well as peptide research. A lot of networking opportunities in a dynamic and friendly atmosphere. Bachem 2013 Highlights 128 20% companies Event growth 189 61% Managers or above attendees Limited Availability: contact [email protected] for more information Who attends • Drug Developers • Researchers • Pharmaceutical Developers • Those in operations • QA & QC • Regulators 2014 floorplan Who should come? • Chemical Developers • Toxicologists • Analysers • HPLC • Peptide/DNA Synthesis • Professionals in Genomics • Biotech firms •L arge, Medium & Small pharmaceutical firms • Suppliers • Diagnostics manufacturers • Consultants • Academics • Regulators Who is already coming Media Partners Sponsorship & Exhibition Opportunities With only 1 stand left time is running out to exhibit at one of Europe’s leading meetings for Peptides and Oligo’s. To enquire about the final stand please contact [email protected] Tel:+44 (0) 207 017 5011 www.informa-ls.com/peptides Agenda Day One: Tuesday 18th November 2014 Back to original programme OPENING PLENARY ADDRESS 08:30 Registration and Morning Coffee 08:50 Opening Remarks from Chairperson 09:00 KEYNOTE: GLP-1 Peptide Engineering Peptides serve as excellent templates for drugs as they possess a unique role in human physiology and pato-physiology. However, endogenously secreted peptides have many limitations when translated into pharmaceuticals. Poor half-life, bioavailability, pharmaco-dynamics, chemical and biophysical stability are common parameters that need to be significantly improved in order to transform a peptide into a convenient drug. Technologies for pharmaceutical peptide engineering and delivery will be reviewed and Novo Nordisk based GLP-1 case stories will be presented. Dr Lars Fogh Iversen, Executive Vice President, Novo Nordisk, Denmark 09:40 KEYNOTE: Oral Bioavailability of Peptides Peptides are considered as inferior drugs for their metabolic instability and low bioavailability. Cyclisation, incorporation of D-amino acids and N-methylation reduce or prevent degradation in gut and serum. In matched cases, N-methylation also conferred oral bioavailability. Structural requirements for a successful N-methylation approach that substantiate the pharmacological properties of the peptides will be presented. Professor Horst Kessler, Emeritus of Excellence, Institute for Advanced Study at the Technische Universität München, Germany 10:20 Panel Discussion: Emerging Trends in Peptide Development • Exploring the current advances in peptide research: Where is the Industry moving? • What does the future hold for peptide science? Panellists consist of speakers from the conference including: r Lars Fogh Iversen, D Executive Vice President, Novo Nordisk, Denmark 11:00 Morning Coffee and Exhibition/Poster Viewing Time STREAM 1: Research & Discovery 11:30 Development of Bicyclic Peptides to Target Protein-Protein Interactions The Bicycle technology is based on repertoires of short peptides displayed on the surface of bacteriophages which can be modified with homo-trifunctional organochemical scaffolds, thus creating large diverse libraries of constrained, bicyclic peptides. These repertoires have been extensively used for iterative selections to identify high affinity binding peptides to a wide array of targets, including receptors, interleukins and proteases. Bicyclic Peptides show antibody-like properties with sub-nanomolar affinities and exquisite selectivities, yet are presented in a 100-fold smaller, chemically synthesised format. The small size enables rapid and efficient extravasation and penetration of tumours. The synthetic nature of Bicyclic Peptides allows for the deliberate modulation and enhancement of metabolic and pharmacokinetic properties, as well as site-specific conjugation to other effector molecules. Results will be presented that exemplify the potential of the technology, the path of chemical development of Bicyclic Peptides, and the application to deliver Bicycle-linked cytotoxic payloads to tumour cells. Dr Dan Teufel, Head of Chemistry, Bicycle Therapeutics, UK 12:05 Disulfide-Rich Peptide Cyclisation. Disulfide-rich peptides such as cyclotides are ultrastable templates that have now been demonstrated to be amenable to incorporate and stabilise around a dozen examples of therapeutically useful peptide sequences. This presentation will describe approaches to mass produce such therapeutic leads using solid phase peptide synthesis, enzyme-mediated cyclisation or plant based production. Professor David Craik, Group Leader, Institute for Molecular Bioscience, University of Queensland, Australia 12:40 Lunch and Exhibition/Poster Viewing Time Back to original programme Agenda Day One: Tuesday 18th November 2014 Back to original programme STREAM 1: Research & Discovery 14:00 Panel Discussion: Comparing the Advantages Between Linear and Cyclic Peptides for Intracellular Delivery • Enabling ease of cellular uptake: How to ensure permeability of cell in drug design • Outlining the considerations for cyclising structures: How to ensure cycle structure? • Is there any evidence for improved intracellular availability? • CMC considerations and challenges need to be considered: - Which structure is easier and more straightforward for development? - Are the physiological characteristics much improved?. Panellists consist of speakers from the conference including: r Waleed Danho, D Former, Distinguished Research Leader, Roche, USA rofessor Horst Kessler, P Emeritus of Excellence, Institute for Advanced Study at the Technische Universität München, Germany rofessor David Craik, P Group Leader, Institute for Molecular Bioscience, University of Queensland, Germany 14:35 Oxytocin: New Interests in a Rather Old Molecule Oxytocin is an endogenous hormone which is currently in clinical use for peripheral indications - mainly labour induction and lactation. Rather recent studies indicate that the central pharmacology of Oxytocin leads to improved social behaviour, making Oxytocin a highly interesting target for potential CNS indications. This lecture will cover our efforts to generate high quality lead peptides and discuss their potential use for autism and related disorders Dr Konrad Bleicher, Medicinal Chemistry, Peptide Area Head, pRED, Roche Innovation Centre Basel, F. Hoffmann-La Roche, Switzerland 15:10The Journey From De-novo Discovery to Pre-clinical Development of IL-6 Peptide Antagonists as Novel Anti-inflammatory Agents To find out more information about this presentation, please visit the conference website at www.informa-ls.com/peptides 15:45 r Dinesh Patel, D President & CEO, Protagonist Therapeutics, USA Afternoon Tea with Exhibition/Poster Viewing Time 16:15 Lessons from an Intranasal, Neuroprotective Peptide, NAPVSIPQ. Why Did It Fail? Davunetide (also known as NAPVSIPQ) is an eight amino acid peptide that stabilises microtubules and in preclinical studies, reverses cognitive dysfunction and improves pathological outcomes. Intranasal was selected as the clinical route of administration and positive Phase 2a data was obtained in two studies, mild cognitive impairment (prodromal Alzheimer disease) and cognitive impairment associated with schizophrenia. A large, 12 month pivotal clinical trial in progressive supranuclear palsy failed to demonstrate any benefit when compared to placebo, and the program was subsequently terminated. A retrospective analysis will be presented on areas of risk and how that risk could have been managed and mitigated with a focus on route of administration, pharmacokinetics and clinical development plans. Dr Bruce Morimoto, Executive Director, Applied Translational Medicine, Celerion, USA 16:50 Highlights From the Development of Linaclotide for the Treatment of Functional Gastrointestinal Disorders Linaclotide is FDA-approved for adults with irritable bowel syndrome with constipation or chronic idiopathic constipation. The orally delivered peptide is the first and only guanylate cyclase-C agonist approved by FDA. Based on nonclinical studies, LINZESS is thought to reduce activity of pain-sensing nerves in the intestine and accelerate gastrointestinal transit. Dr Angelika Fretzen, Vice President of Pharmaceutical Chemistry & Development, Ironwood Pharmaceuticals, USA 17:25 End of Conference Day One followed by Networking Drinks Reception Back to original programme Agenda Day One: Tuesday 18th November 2014 Back to original programme STREAM 2: Development and Manufacturing 11:30 BYRO5 Peptides – Analytical tools In 1997, Lipinski and coworkers described a set of rules for drug-likeness called the rule of 5 (Ro5). The rules define specific limits for molecular weight (MW), counts of hydrogen bond donors and acceptors and the calculated partition coefficient between water and octanol (ClogP) that were important for the pharmacokinetics of drugs in the body. What makes Ro5 violators have good passive permeability is extremely important since an increasing number of pharmaceutically relevant targets bind preferentially compounds that fall Beyond Ro5 space. This talk will be centred on the use of NMR spectroscopy and a novel SFC chromatography method termed EPSA to investigate the strategies to make BYRO5 molecules bioavailable. The interplay of N-methylation strategy and structure will also be presented. Dr Michael Shapiro, Director, Analytical Research Technologies, Pfizer Pharmaceuticals, USA 12:05 Spotlight Presentation This presentation will be hosted by a leading company who operates in the field of peptides. Please contact James Miguel for more information. Email: [email protected], Phone: +44 (0) 207 017 5011 12:40 Lunch and Exhibition/Poster Viewing Time 14:00 Alternative Peptide Delivery Technologies: A Focus on the Oral Route Due to their physicochemical characteristics, peptides are usually administered through the parenteral route, often several times daily. Injectable sustained-release peptide formulations based on biodegradable microparticles or implants have been very successful to enhance patient adherence and convenience, and increase safety and efficacy. They are likely to remain a significant and important part of the new peptide products coming to the market. However, the tremendous developments in alternative non-invasive routes of delivery are likely to result in more and more peptides being delivered by the transdermal, nasal, inhalation and oral routes. The main purpose of this talk will be to analyse and compare the various oral peptide delivery technologies available on the market, focusing on the ones progressing into the clinics. Dr Andy Lewis, Director, Novel Delivery Technologies - CMC & Engineering-Peptides – Technical Operations, Ipsen, France r Joël Richard, D Senior Vice President, Peptides - CMC & Engineering – Technical Operations, Ipsen, France 14:35 Oil-based Formulations for Oral Delivery of Peptides The intestine is designed par excellence for processing of ingested oils, in order to allow them to be taken up into the rest of the body. It is reasonable, therefore, to try to devise delivery vehicles which take advantage of the uptake of oils in the gut, and to use them to deliver peptides via the same route. This talk describes a formulation technology which allows peptides to incorporate in hydrophobic oil phases, and shows some of the successes achieved in eliciting biological responses. Dr Roger New, Co-Founder & Director, Proxima Concepts Ltd, UK Back to original programme Agenda Day One: Tuesday 18th November 2014 Back to original programme STREAM 2: Development and Manufacturing 15:10 Spotlight Presentation This presentation will be hosted by a leading company who operate in the field of peptides. Please contact James Miguel for more information. Email: [email protected], Phone: +44 (0) 207 017 5011 15:45 Afternoon Tea with Exhibition/Poster Viewing Time 16:15Degradation Kinetics & Aggregation Tools: A Combinatorial Approach to Discern Real-Time Formulation Stability of a Pharmaceutical Peptide Aggregation Tools to determine physical stability of Peptides in combination with monitoring of chemical degradation reactions. An approach will be outlined that allows identification of increase in rates of conformation-sensitive chemical reactions upon entering rapid-phase of aggregation. Dr Adrian Podmore, Formulation Scientist, MedImmune, UK 16:50 Panel Discussion: Exploring the Advances in Technology that can Aid Infrequent Dosing of Peptides • What innovations are available to allow infrequent dosing and minimise pain for the patient • Designing peptide drugs with sufficient efficacy in humans to allow infrequent dosing • Outlining the benefits of daily/weekly/monthly dosing and the role that devices can play in this • Delivery systems vs pain release Panellists consist of speakers from the conference including: r Lutz Jermutus, D Senior Director, R&D & Product Development Team Leader, Cardiovascular & Metabolic Diseases iMED, MedImmune Ltd, UK r Matthias Urmann, D Associate Vice President, Research & Translational Medicine, Insulin & Peptides, R&D, Diabetes Division, Sanofi-Aventis Deutschland GmbH, Germany r Oliver Demmer, D Scientist, Medicinal Chemistry, Zealand Pharma, Denmark 17:25 End of Conference Day One followed by Networking Drinks Reception Back to original programme Agenda Day Two: Wednesday 19th November 2014 Back to original programme 08:30 Registration and Morning Coffee 08:55 Opening Remarks from Chairperson STREAM 1: Research & Discovery 09:00 A Lanthipeptide Agonist of the Angiotensin II Type 2 Receptor for Treatment of Fibrosis Lanthipeptides are lanthionine-containing peptides. A lanthionine is composed of two alanines connected by a thioether bridge. The lanthipeptide LP2 shows significant antifibrotic activity in animal models of lung and kidney fibrosis and –directly or indirectly- counteracts cardiac right ventricular hypertrophy. LP2 will enter the clinic early 2015. Dr Gert Moll, CSO, Lanthio Pharma, Netherlands 09:35 Stable D-Enantiomeric Peptides for the Aβ Oligomer Directed Therapy of Alzheimer’s Disease Small soluble Aβ oligomers are suspected to be the major toxic species responsible for disease development and progression of Alzheimer’s disease (AD). We developed a very potent D-enantiomeric peptide compound that specifically eliminates Aβ oligomers, reduces plaque load and inflammation and improves cognitive performance of AD transgenic mice. Professor Dieter Willbold, Director, Institut für Physikalische Biologie, Heinrich-Heine-Universität, Düsseldorf and Director, Institute of Complex Systems, ICS-6: Structural Biochemistry, Research Centre Jülich, Germany 10.10 Engineered Affibody Molecules: Emerging Peptide Drug Candidates for Targeted Therapy Affibody molecules are based on a small protein scaffold. Target-specific candidate drugs with high affinity and specificity are developed and optimised for the intended clinical indication. Fusion of Affibody molecules to (a) the albumin binding domain (ABD) is used to extend the half-life or (b) antibodies to create bi-specific functionalised antibodies (AffiMab’s) with better efficacy. Recent data from our anti-inflammation program will be presented. Dr Joachim Feldwisch, Director Preclinical Development, Affibody, Sweden 10.45 Morning Coffee and Exhibition/Poster Viewing Time 11.15 Antibiofilm Peptides Against the Fungal Pathogen Candida Albicans: Mode of Action and Structure-Activity Relationship The plant-derived decapeptide OSIP108 inhibits biofilm formation of the fungal pathogen C. albicans by interfering with cell wall-related processes. Introduction of positively charged amino acids R, H and K resulted in up to 5-fold increased antibiofilm activity, possibly resulting from their increased interaction with the negatively-charged cell wall. The antibiofilm activity of OSIP108 could be 8-fold increased by combining the most promising amino acid substitutions, i.e. Q6R and G7K. Dr Karin Thevissen, Industrial Research Manager, KU Leuven, Belgium 11.50 Harnessing mRNA-display for the Discovery of Macrocyclic Peptide Drugs Ra’s Extreme Diversity™ peptide discovery platform uses mRNA-display to rapidly synthesise and screen enormous libraries of peptidic macrocycles containing modified backbones and unnatural side-chains. The “hits” from these libraries have excellent affinity and metabolic stability and may be used for the discovery of intracellular protein-protein interaction inhibitors or synthetic replacements for monoclonal antibodies. Dr Kristopher Josephson, Director of Molecular Biology, RA Pharmaceuticals Inc, USA Spotlight Presentation 12.25 This presentation will be hosted by a leading company who operate in the field of peptides. Please contact James Miguel for more information. Email: [email protected], Phone: +44 (0) 207 017 5011 13:00 Lunch and Exhibition/Poster Viewing Time Back to original programme Agenda Day Two: Wednesday 19th November 2014 Back to original programme STREAM 1: Research & Discovery 14.10 Reviewing Effective Techniques for Designing Multi-Specific Acting Peptides Towards Infrequent Dosing For chronic diseases like diabetes, patients still need better and more convenient treatments. Based on the concept of multi-functional peptides, we present hybrid and chimeric peptides that are fine-tuned either towards treatment of diabetes alone or additionally have weight-loss properties. Furthermore, we will show design strategies for infrequent dosing of peptides and to aid their formulation. Dr Oliver Demmer, Scientist, Medicinal Chemistry, Zealand Pharma, Denmark 14:45 Development of Novel Peptide Antibiotics Against Bacterial Biofilms Our lab has designed a new category of cationic antimicrobial peptides (CAPs) that are active against a variety of bacteria and are non-hemolytic in human erythrocytes. Combinations of these CAPs with conventional antibiotics such as tobramycin kill P. aeruginosa biofilms (from cystic fibrosis clinical isolates) with greater efficiency than either drug alone. Professor Charles Deber, Senior Scientist, Division of Molecular Structure & Function, Research Institute, Hospital for Sick Children, Toronto; and Professor, Department of Biochemistry, University of Toronto 15:20 Afternoon Tea and Coffee with Exhibition/Poster Viewing Time 15:50 Discovery and Structure-Based Optimisation of Peptidic and Non-Peptidic Inhibitors Targeting the Adenoviral Protease The adenoviral protease adenain is essential for several critical steps during the adenovirus replication cycle and as such represents a promising target for the treatment adenoviral infections. Screening of a peptide array that mimicked the consensus substrate cleavage site in combination with a focused screen were used to identify starting points for medicinal chemistry. High resolution x-ray co-crystal structures of the initial hits enabled a structure-guided optimisation strategy which resulted in the development of highly potent, drug-like inhibitors of adenain. Dr Eva Altmann, Senior Investigator, Novartis Institute for Biomedical Research, Switzerland 16.25 Exploiting The Biophysical Properties Of Centyrins For Targeted Delivery The biophysical properties of Centyrins make them ideal for conjugation technologies across an array of applications that combine small molecule and large molecules. Centyrex is exploiting this platform via novel therapeutic applications that may address outstanding challenges in antibody drug conjugate technology. The latest results in the design of Centyrin-drug conjugates will be discussed, including their application in targeted nanoparticle technology. Dr Vadim Dudkin, Associate Director, Centyrex, Janssen R&D, USA 17:00 Closing Remarks from Chairperson 17:10 End of Conference STREAM 2: Development and Manufacturing 09:00 Therapeutic Peptides through Synthesis, Recombinant Expression and Bioconjugation To find out more information about this presentation, please visit the conference website at www.informa-ls.com/peptides Dr Lutz Jermutus, Senior Director, R&D & Product Development Team Leader, Cardiovascular & Metabolic Diseases iMED, MedImmune Ltd, UK 09:35 Chemical Synthesis of Peptide Macrocycles Cyclised peptides with constrained conformation have significant diagnostic and therapeutic potential. Case studies comprising manufacturing of peptides with ring sizes from 5 to 17 amino acids and different cyclisation strategies will be presented. We will showcase structure elucidation of an unexpected impurity detected during production of a bicyclic peptide containing a head-to-tail lactam and a di-sulfide bond and address subsequent manufacturing process optimisation. Dr Thomas Meier, Vice-President Production, Bachem AG, Switzerland Back to original programme Agenda Day Two: Wednesday 19th November 2014 Back to original programme STREAM 2: Development and Manufacturing 10:10 Assessing the Applications of Microwave Assisted Solid Phase Peptide Synthesis The growing number of peptides entering the market is a result of impressive advances in peptide research in the last decade. From our perspective the implementation of microwave assisted synthesis was one of the most remarkable breakthroughs - not caused by a microwave effect, but by simply enabling us to synthesise even challenging cell-penetrating peptides for targeting tumor stemness using standard protocols without time consuming optimisation. Dr Andreas Rybka, Head of Peptide Chemistry, Nexigen GmbH, Germany 10:45 Morning Coffee and Exhibition/Poster Viewing Time 11:15 Solid-Phase Peptide Synthesis: Microwave Heating and New Reagents Solid-phase peptide synthesis (SPPS) has been very successful both in academia and industry. However, SPPS still faces many limitations. Here we describe the development of new reagents and methods to reliably use microwave heating in SPPS. Dr Knud Jensen, Professor of Nanobioscience, Department of Chemistry, University of Copenhagen, Denmark 11:50 Current and Future Challenges of Peptide Manufacturing To find out more information about this presentation, please visit the conference website at www.informa-ls.com/peptides Dr Jon Rasmussen, Director, Global Development, PolyPeptide, Denmark 12:25 Panel Discussion: Synthetic versus Recombinant Techniques for Peptide Synthesis? • What are the advantages and disadvantages for each technique? •Assessing the differences in product types •What considerations are required for effective process development? •Ease of scale up •Cost implications for each strategy Panellists consist of speakers from the conference including: r Thomas Meier, D Vice-President Production, Bachem AG, Switzerland r Jon Rasmussen, D Director, Global Development, PolyPeptide, Denmark 13:00 Lunch and Exhibition/Poster Viewing Time 14:10 Investigating Molecular Technologies that can Extend Peptide Half-Life To find out more information about this presentation, please visit the conference website at www.informa-ls.com/peptides Dr Cyrille Gineste, Chief Scientific Officer, Riogin Corp, USA 14:45 Spotlight Presentation This presentation will be hosted by a leading company who operate in the field of peptides. Please contact James Miguel for more information. Email: www.informa-ls.com/peptides, Phone: +44 (0) 207 017 5011 Back to original programme Agenda Day Two: Wednesday 19th November 2014 Back to original programme STREAM 2: Development and Manufacturing 15:20 Afternoon Tea and Coffee with Exhibition/Poster Viewing Time 15:50PASylation: A Uniform Biosynthetic Polymer with PEG-Like Biophysical Properties for the Development of Peptides and Proteins with Enhanced Action Short circulation is a major draw-back of most biopharmaceuticals, in particular peptides. PEGylation is now widely applied, but has disadvantages with regard to polydispersity and accumulation in tissues. PASylation allows the facile conjugation with a voluminous hydrophilic and biodegradable Pro/Ala-rich sequence of natural L-amino acids as an efficient alternative technology to retard kidney filtration and design better drugs with extended half-life. Dr Lars Friedrich, Scientist, XL-Protein GmbH, Germany 16:25 XTEN – A Biodegradable Alternative to PEG for Half-Life Extension and Drug Delivery Amunix’s half-life extension technology is based on XTEN, an unstructured protein-based polymer with PEG-like properties. Highly-pure XTEN polymer can be produced in high-yield microbial fermentation enabling the chemical XTENylation of peptides and other active moieties. XTEN is monodisperse, allowing for efficient process development and conjugation monitoring by mass spectrometry. The inclusion of thiol and/or amino groups in pre-defined locations enables the generation multispecific as well as multivalent XTENylated products with precise control of payload number and spacing. A variety of XTENylated pharmaceuticals is currently in clinical as well as preclinical development. Dr Volker Schellenberger, President and CEO, Amunix Operating Inc., USA 17:00 Closing Remarks from Chairperson 17:10 End of Conference Back to original programme
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