PEGS Europe Summit Biologics Dev Stream

Cambridge Healthtech Institute’s Sixth Annual
Optimisation and Development of Biologics

Strategies for Candidate Selection and Enhancement of Product Properties

2-3 November 2015

This track on Optimisation and Development of Biologics presents an exciting range of approaches for new biotherapeutics and those already under development. Big pharma and the larger biotechs will present their strategies and approaches to enable attendees to work out how to do the right thing at the right time in order to avoid hurdles further down the line.

This track presents strategies for selecting products with unique characteristics, and for optimisation of affinity, specificity, potency and clearance, and minimisation of side effects. It presents delivery approaches to enhance targeting of specific tissues, optimisation of formulation and manufacture, and preclinical evaluation.

Final Agenda

Day 1 | Day 2 | Speaker Biographies | Download Brochure

Unpublished Data Icon: Unpublished Data | Case Study Icon: Case Study



Monday 2 November

12:00 Conference Registration



13:40 PEGS Europe Team Welcome

13:45 Chairperson’s Opening Remarks

Darrell_SleepDarrell Sleep, Director, Novozymes Biopharma R&D


13:50 Protein Engineering for New Modes of Actions and New Targets

Andreas G. PlückthunAndreas G. Plückthun, Ph.D., Professor & Director, Biochemistry, University of Zurich

Using different display technologies and structure-based engineering, the possibilities of hitting extra- and intracellular targets will be discussed, with an emphasis on extending the modes of action previously possible. The lecture will emphasise the need for interdisciplinary approaches.

14:30 Targeting Ion Channels

Tristan J. VaughanTristan J. Vaughan, Ph.D., Vice President, R&D, Antibody Discovery & Protein Engineering, MedImmune Ltd.

Ion channels are complex integral membrane proteins that form a pore through which ions selectively pass down an electrochemical gradient. They are prominent components of the nervous system where they can mediate transduction across synapses. Hence, certain channels represent good drug targets, especially for alleviating pain. Approaches will be described to target such ion channels with antibody-based drugs and a case study presented.

15:10 Current and Future Trends in Antibody Therapeutics

Parren PaulPaul W.H.I. Parren, Ph.D., Senior Vice President & Scientific Director, Preclinical Development & Research, Genmab

Targeted treatment using antibody therapeutics has proved successful in the development of meaningful treatments in diverse therapeutic areas. However, despite strong advances, many patients still fail to respond or become resistant to targeted treatment and novel innovative approaches to improve therapy are therefore required. Genetic and chemical engineering of antibodies, fueled by recent molecular insights, is providing important opportunities for the development of more potent antibody therapeutics. Examples from Genmab’s portfolio will be provided.

15:50 Refreshment Break in the Exhibit Hall with Poster Viewing



16:30 Chairperson’s Remarks

William Finlay, Ph.D., Senior Director, Global Biotherapeutics, Pfizer, Inc.

Case Study and Unpublished Data Icon
Fischer Fischer
16:35 Purpose Oriented Antibody Libraries for de novo Generation of pH-Dependent Antibodies

Nicolas Fischer, Ph.D., Head, Research, Novimmune SA

Some antibodies having unique characteristics such as pH-dependent antigen binding are difficult to isolate using standard antibody generation platforms and thus require extensive engineering. We have created several purpose-oriented antibody libraries to facilitate the de novo isolation of candidates with characteristics such as pH-dependent binding or enzyme neutralisation activity.

Case Study and Unpublished Data Icon
Finlay William
17:05 Augmented Binary Substitution: Simultaneous Ultra-Humanisation, CDR Redundancy Minimisation and Stabilisation of Antibodies for Human Therapy

William Finlay, Ph.D., Senior Director, Global Biotherapeutics, Pfizer, Inc.

This study presents a technology that generates stable, soluble, ultra-humanised antibodies via single-step CDR redundancy minimisation. For three antibodies from three separate key immune host species, ABS processing significantly lowered non-human sequence content, minimised T and B cell epitope risk in the final molecules and provided a heat map for the essential non-human CDR residue content of each antibody.

Novozymes Cropped17:35 Veltis® Technology: Engineered Albumins for Optimized Serum Half-Life Extension

Hay_JoannaJoanna Hay, Ph.D., Customer Solution Science Manager, Novozymes Biopharma UK

Short circulatory half-life represents a major obstacle for many protein and peptide-based therapeutics, resulting in increased dosing with the consequent risk of side effects and reduced patient compliance. The half-life of therapeutic can be significantly improved by conjugation or fusion to albumin, due to both size and recycling via the neonatal Fc receptor (FcRn). We will describe rationally engineered albumins with increased FcRn affinity and their application to improve the pharmacokinetic properties of therapeutic candidates.

18:05 Welcome Reception in the Exhibit Hall with Poster Viewing

19:05 End of Day One

Day 1 | Day 2 | Speaker Biographies | Download Brochure



Tuesday, 3 November

07:45 Registration and Morning Coffee



08:30 Chairperson’s Remarks

Fischer Fischer

Nicolas Fischer, Ph.D., Head, Research, Novimmune SA

Case Study Icon
Tissot Alain
08:40 Design of Bispecific Antibodies: Target Biology Determines Optimal Valency of Binding Sites

Alain C. Tissot, Ph.D., Head, Immune Biology, Large Molecule Research, Pharma Research and Early Development, Roche Innovation Center, Penzberg

Bispecific antibodies are attractive for multifactorial diseases and simplify development over combination therapies, particularly when the targets are two ligands. We provide data for two preclinical bispecific antibodies in RA targeting ligands, demonstrating the value of varying the valency of binding sites in order to fully exploit target biology and potency.

Case Study and Unpublished Data Icon
Heinis Christian
09:10 Exploiting the Advantages of Bicyclic Peptide Therapeutics

Christian Heinis, Ph.D., Professor, Institute of Chemical Sciences and Engineering, Ecole Polytechnique Federale de Lausanne (EPFL)

My laboratory is developing antagonists based on bicyclic peptides by phage display. The bicyclic peptides combine key qualities of antibody therapeutics (high affinity and specificity) and advantages of small molecule drugs (access to chemical synthesis, diffusion into tissue, various administration options). An update on recently developed bicyclic peptides and their activities will be given.


Table 4: Alternative Protein Scaffolds: Lessons from the Past and Future Expectations

Moderator: Christian Heinis, Ph.D., Professor, Institute of Chemical Sciences and Engineering, Ecole Polytechnique Federale de Lausanne (EPFL)

Table 5: Engineering for Optimization

Moderator: Laura Lin, Ph.D., Director, Global BioTherapeutic Technologies, Pfizer, Inc.

Table 6: Improving Therapeutic Antibody Formats

Moderator: Paul W.H.I. Parren, Ph.D., Senior Vice President & Scientific Director, Preclinical Development & Research, Genmab B.V.

10:40 Coffee Break in the Exhibit Hall with Poster Viewing



Case Study and Unpublished Data Icon
Murata Erico
11:20 pH and Calcium-Dependent Fully Human Biparatopic IgG Antibody for Efficient Elimination of Soluble Antigen from Plasma

Eriko Murata, Master of Pharmacy, Research Scientist, Discovery Research, Chugai Pharmaceutical Co. Ltd.

We have previously shown that calcium-dependent antigen-binding antibody increases soluble antigen elimination by dissociating the antigen in the endosome. Here we report on a novel strategy to further accelerate antigen elimination from plasma in vivo. Identification and optimisation of calcium-dependent binding biparatopic antibody which forms multimeric antibody-antigen complexes to enhance binding to Fc receptors will be presented.

Case Study and Unpublished Data Icon
Peter Ulrichts
11:50 ARGX-113, A Novel Fc -Based Therapeutic Approach for Antibody-Induced Pathologies

Peter Ulrichts, Ph.D., Senior Scientist, ArGEN-x

ARGX-113 is a proprietary antibody fragment based on arGEN-X’ ABDEG™ technology. ARGX-113 works by preventing pathogenic autoantibodies from being recycled, promoting their degradation and thereby clearing them from circulation. Preclinical data in cynomolgus monkeys proved ARGX-113 to be highly effective in rapidly eliminating pathogenic antibodies, while sparing the broader immune response. The data support further clinical development of this novel therapeutic approach in autoimmune disease management.

12:20 Epitope Binning, Mapping and Affinity Ranking of 96 Antibody Supernatants

Richard_SchasfoortRichard B.M. Schasfoort, Ph.D., CSO, IBIS Technologies B.V.

The binding of an antibody to an epitope is innate and cannot be engineered anymore. Therefore the selection of antibodies that bind to the right functional epitope should be carried out as early as possible. Technology is now available enabling binning, mapping and affinity ranking of up to 96 Ab-sups in one unattended run.

12:50 Luncheon Presentation (Sponsorship Opportunity Available) or Lunch on Your Own

13:20 Session Break

14:00 Desert Break in the Exhibit Hall with Poster Viewing



14:30 Chairperson’s Remarks

Frank Walsh, CEO, Ossianix and Professor, Kings College London

Case Study and Unpublished Data Icon
Lin laura
14:35 Early Stage Developability Assessment of Biotherapeutics

Laura Lin, Ph.D., Director, Global BioTherapeutic Technologies, Pfizer, Inc.

The presentation will describe an early stage molecular assessment platform we established in-house to rank, select, and optimise biotherapeutic leads in early discovery at Pfizer. I will be discussing our strategies of early screening for biophysical properties for a given project, and triage down a few leads for more in-depth developability assessment. I will share a specific case study highlighting developability comparisons between different modalities and the impact on efficacy, PK, and manufacturability.

Case Study and Unpublished Data Icon
Moore Paul
15:05 Preclinical Development of MGD010: A CD32BxCD79B Bispecific DART for the Treatment of Autoimmune Disease.

Paul Moore, Ph.D., Vice President, Research, Cell Biology & Immunology, MacroGenics, Inc.

MGD010, a bi-specific Dual-Affinity ReTargeting (DART) that inhibits B-cell activation via colligation of the inhibitory FcγRIIb receptor CD32B with the BCR component CD79B, is being developed as a novel therapeutic molecule for autoimmunity. Studies performed to support MGD010 clinical development will be presented, covering mechanism of action, therapeutic modeling, safety pharmacology and first-in-human dose projection

15:35 Preclinical Studies with FynomAbs, Fynomer-Antibody Fusion Proteins

Vanessa Baeriswyl, Ph.D., Scientist, Covagen AG, one of the Janssen Pharmaceutical Companies of J&J

Bispecific FynomAbs are generated by fusing Fynomer binding proteins to antibodies. The ability to fuse Fynomers to multiple sites on the antibody allows the creation of therapeutics with higher potency and desired bioactivity, since the efficacy of bispecifics is greatly influenced by the orientation of the two binding sites relative to each other. Case studies of FynomAbs having selective tumour killing properties will be presented, as well as key parameters, such as manufacturability and yield (3.3 g/l obtained in 1000 liter GMP run), pharmacokinetics and stability.

16:05 Computational Advances in Antibody Design: Toward Improved Optimization and Selection

Pearlman_DavidDavid Pearlman, Ph.D., Biologics, Schrödinger

Recent computational advances hold significant promise both for improved prediction of antibody structure from sequence, and for the ability to precisely calculate physically relevant properties such as affinity and stability. When combined with additional theoretical approaches to identify liabilities, we can use these tools to variously optimize a lead antibody candidate and triage among multiple potential leads.

16:35 Refreshment Break in the Exhibit Hall with Poster Viewing



Case Study and Unpublished Data Icon
Michael Siedler
17:15 Implementation of an Integrated High-Throughput Formulation Screening for Biologics

Michael Siedler, Ph.D., Section Head, NBE Formulation Sciences & Process Development, AbbVie Deutschland GmbH & Co KG

Modern formulation development increasingly relies on multivariate parameter analysis in order to enable statistical analysis. Consequently, the only way to generate and leverage the required vast amount of data is by applying appropriate scale-down methodologies and lab automation in conjunction with an IT infrastructure capable of transforming the data into knowledge. We will provide a case study of how this can be achieved.

Unpublished Data Icon
Walsh Frank
17:45 Delivery of Single Domain Antibody Biotherapeutics to the Brain (NAB)

Frank Walsh, CEO, Ossianix and Professor, Kings College London

This presentation will describe the development of a toolkit of individual single domain VNAR antibodies to the transferrin receptor 1 that bind with varying affinities to multiple epitopes on the receptor. These allow the generation of bispecific biotherapeutics that will cross the BBB via receptor-mediated endocytosis at therapeutic doses and can be tailor-made for differing therapeutic modalities. Studies showing direct translation from animal data to humans will be included.

Unpublished Data Icon
Mathieu Cinier
18:15 Oral Delivery of Anti-TNF-Alpha Nanofitin Shows a Strong Preventive and Curative Anti-Inflammatory Effect in Models of Inflammatory Bowel Diseases

Mathieu Cinier, Ph.D., Scientific Director, Affilogic

Despite remarkable efficacy, treatment of IBD using systemic administration of anti-TNF-alpha antibodies remains associated with serious adverse effects. Extreme stability of the Nanofitins, novel alternative scaffolds, in the gut environment enable the development of orally available anti-TNF-alpha therapeutics and allow better targeting of the inflammation site while decreasing systemic exposure and related side effects.

18:45 End of Optimisation & Development


Day 1 | Day 2 | Speaker Biographies | Download Brochure

Unpublished Data Icon: Unpublished Data | Case Study Icon: Case Study