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Next Generation Protein Therapeutics Summit

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Cross-Fertilize Ideas from Multiple Disciplines and Turn Promising New Molecules into Differentiated Products

June 04-06, 2014
Grand Hyatt Hotel
San Francisco, CA

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Alternative Language Options:

  • Japanese
  • Korean
  • Taiwanese
  • Chinese

Agenda

Agenda

Wednesday, June 4, 2014

7:00
Registration and Coffee

8:00
Chairman's Opening Remarks
Jonathan Davis, Ph.D., Principal Scientist, Molecular Structure and Design, Bristol-Myers Squibb

Keynote Presentations

8:15
Unpublished Data
Carolyn R. Bertozzi, Ph.D. Bioorthogonal Chemistries for Biomolecular Engineering
Bioorthogonal chemical reactions have such exquisite selectivity that they can be employed to modify biomolecules even within the environs of live organisms. This presentation will focus on recent developments in bioorthogonal reaction methodology and applications to the production of chemically modified protein therapeutics such as antibody-drug conjugates. The use of bioorthogonal chemical reporters for in vivo imaging and disease biomarker discovery will also be discussed.
Carolyn R. Bertozzi, Ph.D., T.Z. and Irmgard Chu Distinguished Professor of Chemistry and Professor of Molecular and Cell Biology, UC Berkeley; Investigator, Howard Hughes Medical Institute; Senior Faculty Scientist, Lawrence Berkeley National Laboratory

8:45
Unpublished Data
Karl Dane Wittrup, Ph.D. Does Targeting Contribute to Immunocytokine Efficacy?
Immunocytokines are fusions of antibodies to immunostimulatory cytokines that can exhibit greater anti-tumor efficacy than the parent antibody. However, the cytokine component of an immunocytokine may systemically activate immune cells, leading both to potential systemic toxicity or contributions to efficacy. We have performed simple pharmacokinetic analyses that provide quantitative design objectives for immunocytokines.
K. Dane Wittrup, Ph.D., Professor, Chemical Engineering & Biological Engineering, MIT

9:15
Robert Lutz, Ph.D. The Evolution of ADCs: Lessons Learned from the Past. Where are We Going?
This talk will cover what has been learned in the two decades of ADC clinical development. It will highlight the problems encountered with current technologies and discuss where new technologies, such as site directed conjugation, alternate scaffolds, and new payloads may provide answers (or new problems!).
Robert Lutz, Ph.D., Vice President, Translational Research and Development, ImmunoGen, Inc.

9:45
Networking Refreshment Break in Poster & Exhibit Hall

Scaffolds at the Frontier of Biologics

10:30
Unpublished DataCase Study
Creating Differentiated Therapies using Affibody Technology
Affibody molecules are developed to address significant unmet medical need. Their small size and high potency is key to differentiation, and in addition allows novel multispecific antibody-based drugs to be developed. Enhanced Pk with a clinical stage albumin binding domain results in efficient blocking of inflammatory disease, an unpublished translational case study will be presented.
Fredrik Frejd, Ph.D., Chief Scientific Officer, Affibody AB, Sweden

11:00
Unpublished DataCase Study
Breaking New Therapeutic Grounds using Multi-Functional DARPins
The DARPin platform allows for the design of powerful drugs combining multiple functionalities. Such combinations enable novel therapeutic concepts with improved efficacy and PK as well as mechanism of action tailored to optimally address diseases with unmet medical needs. We will present examples from our clinical and preclinical programs that have the potential to surpass current standards of care or break new therapeutic ground.
H. Kaspar Binz, Ph.D., Vice President and Co-Founder, Molecular Partners AG, Switzerland

11:30
Unpublished Data
Ultra-High Affinity Engineered Protein Therapeutics for Treating Metastatic Disease
A soluble receptor was used as a therapeutic strategy to inhibit the biological activity of a ligand involved in cancer metastasis. Combinatorial and rational methods were used to engineer variants that bound ligand with affinities in the femtomolar range. The engineered receptors exhibited a remarkable ability to inhibit cancer metastasis in several aggressive tumor models in contrast to the wild-type receptor which was only marginally effective.
Jennifer Cochran, Ph.D., Associate Professor of Bioengineering and Chemical Engineering, Stanford University

12:00
Unpublished DataCase Study
Preclinical Development of an Anti-IL-23 Adnectin and Advancement into the Clinic
We describe the identification of p19-specific Adnectins against the inflammatory cytokine, IL-23 with subnanomolar binding to human and non-human primate targets and potent inhibition of IL-23 induced cytokine production in primary cells. Following PEG-ylation for pharmacokinetic enhancement a lead Adnectin (BMS-938790) was progressed to in vivo studies. We present the pharmacokinetic and bioavailability assessment in mice as well as inhibitory activity in a pharmacodynamic model. BMS-938790 demonstrated efficacy in the marmoset experimental autoimmune encephalomyelitis by reducing the onset and severity of clinical symptoms. Finally, BMS-938790 displayed favorable pharmacokinetics in a dose escalation study in normal healthy volunteers.
Ruchira Das Gupta, Ph.D., Associate Director, Molecular Discovery Technologies, Bristol-Myers Squibb

12:30
Networking Luncheon in the Poster & Exhibit Hall

1:40
Chairman's Remarks
Peter Kiener, Ph.D., Chief Scientific Officer, Ambrx

Bispecific and Multivalent Approaches

1:45
Unpublished DataCase Study
FynomAbs: Taking Antibodies to the Next Level
Covagen develops bispecific FynomAbs by fusing its human Fynomer binding proteins to antibodies resulting in therapeutics with enhanced efficacy. We present COVA322, a bispecific anti-TNF/IL-17A FynomAb, which blocks the activity of both cytokines in vitro and in vivo with picomolar inhibition potencies. COVA322 exhibits excellent biophysical properties and has been produced under GMP conditions with a yield of 3.3g/l (1000l scale) using standard antibody production methods.
Dragan Grabulovski, Ph.D., Chief Scientific Officer, Covagen AG, Switzerland

2:15
Unpublished Data
Multimeric Anticalin® Fusion Proteins with Novel Binding and Targeting Properties
Anticalins® are ~18 kD protein therapeutics derived from human lipocalins and enable straight-forward multimeric drug targeting across several formats. Multimeric binders are generated by, e.g., fusing multiple distinct Anticalins® to each other or to mAb-based moieties. This flexibility allows fine-tuning of valency, avidity, specificity for two or more targets and half life. Applications in autoimmunity and tumor immunotherapy are presented.
Ulrich Moebius, Ph.D., Chief Scientific Officer, Pieris AG, Germany

2:45
Unpublished DataCase Study
Towards Reproducibility in Discovery and Engineering of Bispecific Antibody Therapeutics
The use of a single human variable domain scaffold allows for the reproducible engineering of highly stable and potent humanized rabbit antibody variable domains. Such variable domains are used as building blocks for the engineering of bispecific single-chain diabodies (scDb) with excellent CMC properties. Numab is exploiting bispecific scDbs with T killer cell redirecting activity for the therapy of chronic inflammatory diseases.
David Urech, Ph.D., Co-CEO and Chief Scientific Officer, Numab, Switzerland

3:15
Networking Refreshment Break in Poster & Exhibit Hall

4:00
Unpublished DataCase Study
Novel Engineering Solutions to the "Common Light Chain Problem" Give Rise to Potent Bispecifics with Favorable Developability Profiles
A variety of bispecific constructs employing modifications in the Fc region benefit from the use of a single common variable light region (VL) capable of pairing with two different variable heavy regions (VHs) for bi-functional targeting. We report here the engineering of multiple VHs that pair with a single light chain against three targets with unrelated epitopes. Bispecific constructs were generated with a common light chain that bind to each target with low picomolar affinities and exhibit favorable biophysical properties similar to benchmarks established by traditional mAbs.
Robert Mabry, Ph.D., Associate Director, Antibody Discovery and Bispecific Engineering, Adimab, LLC

4:30
Unpublished DataCase Study
Preclinical Developments with a Fully Human Bispecific Antibody Platform
This presentation will describe a platform technology to generate fully human bispecific antibodies through the combination of Fc modifications that allow selective protein A purification and VelocImmune® derived antibodies that utilize a single defined light chain. Molecular characterization and initial in vitro efficacy data will be discussed. In addition, pre-clinical findings with proof-of-principle molecules targeting T-cells will be presented.
Eric Smith, Ph.D., Associate Director, Bispecifics, Regeneron Pharmaceuticals

5:00
Unpublished DataCase Study
A Novel Bispecific Antibody-Receptor Domain Fusion Protein that Simultaneously Targets IGF-IR and VEGF for Degradation in Tumor Cells
A fully human Bispecific Antibody-receptor domain (VEGFR1 domain 2) fusion molecule with ligand Capture (BiAbCap) targeting IGF-IR and VEGF was designed and developed. BiAbCap represents a novel and developable format of bi-functional antibodies with potent neutralizing activities against both targets. The unique "capture-for-degradation" mechanism translates to potent anti-tumor activity superior to the combination in vivo.
Yang Shen, Ph.D., Director, Antibody Technology, ImClone Systems, a wholly-owned subsidiary of Eli Lilly and Company

5:30
Networking Cocktail Reception in Poster & Exhibit Hall

Thursday, June 5, 2014

7:30
Coffee

Track A

8:00
Chairman's Opening Remarks
Robert Mabry, Ph.D., Associate Director, Antibody Discovery and Bispecific Engineering, Adimab, Inc.

Creative Protein Engineering and Design Approaches

8:15
Unpublished DataCase Study
Deep Sequencing Guided Engineering of Affinity and Stability of a Dual Action Fab to Obtain In Vivo Efficacy
We set out to generate a dual action Fab(DAF) against two soluble antigens with high dual affinity. To improve the DAF we used an approach, which combines affinity based selection on phage with deep sequencing. Through this approach we generated several variants of DAF, which possess sub-nanomolar affinity for both antigens as well as higher thermo stability. The improved variants now showed improved efficacy in an animal gating model. Further, mapping the optimized variants with structural data of the DAF in complex with both antigens allows us to deduce improved strategies for maturation library design in the future.
Patrick Koenig, Ph.D., Postdoctoral Research Fellow, Antibody Engineering, Genentech, Inc.

8:45
Unpublished Data
Efficient Design and Engineering of Bi- and Tri-Specific DART Proteins
A challenge in developing robust and stable complex biologics such as bispecifics and ADCs is ensuring that the component elements assemble correctly in a homogeneous manner and that undesired side-products are minimized in the final product. This presentation will focus on design and engineering elements that are incorporated into production of bi- and tri-specific DART proteins, focusing on longer half-life versions.
Syd Johnson, Ph.D., Vice President, Antibody Engineering, MacroGenics, Inc.

9:15
Unpublished Data
Rapid High-Resolution Functional Epitope Mapping of Antibodies Using Yeast Surface Display and Deep Sequencing
Here we demonstrate the functional epitope mapping of a panel of Staphylococcus aureus alpha toxin neutralizing antibodies with a level of speed and precision never seen before by using a rationally designed library, yeast surface display and high throughput DNA sequencing. This approach also produces quantitative insights into the antibody-antigen interaction which was exploited to select antibodies for oligoclonal therapy.
Thomas Van Blarcom, Ph.D., Principal Scientist, Protein Engineering, Pfizer Inc.

9:45
Networking Refreshment Break in Poster & Exhibit Hall

10:30
Unpublished Data
Design Principles for Bispecific IgGs - The H-L Pairing Challenge
Bispecific IgGs are preferably of the IgG format. One of the key challenges in making bispecific IgGs is correct H-L chain pairing. We present a solution, disulfide stabilization, where an engineered disulfide bond H and L chains replaces the natural disulfide bond between the CH1 and CL domains. We efficiently produce several such bsAbs in bacteria and in mammalian cells.
Itai Benhar, Ph.D., Professor, Molecular Microbiology and Biotechnology, Tel-Aviv University, Israel

11:00
Unpublished Data
Engineering of Strong Erbb2-Binders with Adaptable Albumin-Binding
I will describe in detail how we have generated high affinity binders to ErbB2 and how we achieve a unique flexibility to switch between a monospecific target-binding molecule and a bispecific form that also binds albumin. This allows convenient adaptation to a format suitable for molecular imaging or therapy. The first and very promising in vivo data of an ErbB2-binding variant with sub-nanomolar affinity were recently acquired. I will here for the first time present initial data on tumor imaging using this scaffold.
Johan Nilvebrant, Ph.D., Post Doctoral researcher, Protein Technology, Royal Institute of Technology - Biotechnology, Sweden

11:30
Unpublished Data
Novel Asymmetrically Engineered Antibodies with Unique Functions
Two examples for asymmetric antibody engineering enabling unique functions that cannot be achieved by conventional antibody will be presented. One is asymmetric Fab engineering to design bispecific antibody against FIX and FX mimicking FVIII function, which is being investigated in Phase 2. Second is asymmetric Fc engineering to fine-tune the asymmetric Fc-FcgR interaction for maximizing FcgR binding affinity and ADCC.
Futa Mimoto, Researcher, Research Division, Chugai Pharmaceutical Co., Ltd, Japan

12:00
Unpublished Data
Application of In Vitro V(D)J Recombination to Generate Peptide-Grafted Antibodies to G Protein-Coupled Receptors
A novel strategy to place sequences encoding GPCR-targeting peptides into the CDRs of full length human antibodies is presented. Utilizing RAG-mediated V(D)J recombination for the generation of large de novo libraries of peptide-grafted antibodies allows for the simultaneous diversification of the length and amino acid composition of flanking antibody-peptide junctions. Peptide-grafted antibodies have the potential to extend the in vivo half-life of peptides and to protect them from proteolytic processing improving their utility as therapeutics.
Michael Gallo, Ph.D., President, Discovery, Innovative Targeting Solutions, Inc.

Track B

8:00
Chairman's Opening Remarks
Dragan Grabulovski, Ph.D., Chief Scientific Officer, Covagen AG, Switzerland

Constraining Peptides for More Drug Like Properties

8:15
Unpublished DataCase Study
Development of Bicyclic Peptides for Therapeutic Application
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). We have developed bicyclic peptide antagonists or ligands with nanomolar or even picomolar binding affinity to a range of important disease targets. First studies in mice show that they are stable and active in vivo.
Christian Heinis, Ph.D., Assistant Professor, Institute of Chemical Sciences and Engineering, Ecole Politechnique Fédérale de Lausanne (EPFL), Switzerland

8:45
Unpublished Data
Ribosomal Synthesis and Discovery of Constrained Peptides and Pseudo-Natural Products
We have developed RaPID system that enables for the ribosomal synthesis and discovery of constrained macrocyclic peptides from over a trillion of members of such peptides. We also recently devised the next generation system consisting of RaPID system and post-translational modifying enzymes. I shall provide a sneak preview of this technology.
Hiroaki Suga, Ph.D., Professor, The University of Tokyo, Japan

9:15
Unpublished Data
Design and Development of Stapled Peptides Activating p53 for Cancer Therapy
This presentation discusses the structure-based discovery of stapled a-helical peptide having potent and selective biological activities: ATSP-7041, a dual MDM2/MDMX inhibitor, achieves sub-micromolar in vitro activity, and demonstrates robust tumor growth suppression in Xenograft models. ATSP-7041 is a precursor to a more potent molecule that is undergoing IND enabling studies and is planned for entry into clinical trials in 2014.
Vincent Guerlavais, Ph.D., Distinguished Scientist, Aileron Therapeutics

9:45
Networking Refreshment Break in Poster & Exhibit Hall

Development of Immunotherapies

10:30
Bi- and Tri-Functional Antibody-Cytokine Fusion Proteins for Cancer Immunotherapy
Cytokines with immunostimulatory/costimulatory properties have shown great potential to support the generation and development of an antitumor immune response. In order to improve the efficacy of such molecules at the tumor site we designed bi- and tri-functional antibody-cytokine fusion proteins, focusing on targeted presentation and a combined mode of action, demonstrating enhanced immune responsiveness in vitro and antitumor activity in vivo.
Dafne Müller, Ph.D., Group Leader, Institute of Cell Biology and Immunology, University of Stuttgart, Germany

11:00
Blinatumomab - History, Mechanism Clinical Update, and Future Path of BiTe Technology
Abstract not available at time of print.
Tap Maniar, MD, Medical Director, Oncology, Amgen Inc.

11:30
Unpublished Data
Engineering Human MICA as a Novel Immunotherapeutic Scaffold
Natural Killer (NK) cells employ the NKG2D receptor to seek and destroy cancerous or virally infected cells displaying the NKG2D activating ligand, MHC-I related chain A (MICA). New data will be presented describing the development of MICA into an immunotherapeutic scaffold by engineering both target antigen binding and NK effector recruitment properties. These agents, termed Micacides, offer an NK cell-directed approach for treating cancer and viral diseases.
Kyle Landgraf, Ph.D., Senior Scientist, Immunotherapeutics, AvidBiotics Corp.

12:00
Spotlight Presentation to be Announced
For more information on spotlight presentations, please contact Patty Rose at (508) 614-1406 or prose@ibcusa.com

12:30
Networking Luncheon in Exhibit and Poster Hall with "Hot Topic" Roundtable Discussions
Moderated by Conference Speakers - Join us during this afternoon's luncheon for informal, moderated hot topic discussions led by your conference speakers. Discuss and debate important industry issues and challenges with other attendees and speakers and make new contacts at the same time.
  • Delivery Approaches for Intracellular Biologics
    Moderator: Paul Watt, Ph.D., Chief Scientific Officer, Phylogica Ltd., Australia
  • Engineering Therapeutic Proteins for Optimized Plasma Half-Life
    Moderator: Arne Skerra, Ph.D., Chief Scientific Officer, XL-protein GmbH, Germany
  • Peptides as Drugs?
    Moderator: Dragan Grabulovski, Ph.D., Chief Scientific Officer, Covagen AG, Switzerland
  • Assessing and Mitigating Immunogenic Risk: What Factors are Worth Considering?
    Moderator: Jonathan Davis, Ph.D., Principal Scientist, Protein Design, Bristol-Myers Squibb
  • Small is Beautiful - What Half-Life Extension Technology Offers the Best Bang for the Buck?
    Moderator: Fredrik Frejd, Ph.D., Chief Scientific Officer, Affibody AB, Sweden

1:40
Chairman's Remarks
Arne Skerra, Ph.D., Managing Director & Chief Scientific Officer, XL-protein GmbH, Germany

Next Generation ADCs - Novel Conjugation Technologies, Linkers and Payloads

1:45
Unpublished DataCase Study
Advances in Drug Conjugate Technology Using Centyrin Proteins
Centyrex has designed a novel FN3 domain alternative scaffold with superior stability properties and is exploring the robustness of the platform via novel therapeutic applications that may address outstanding challenges in antibody drug conjugate technology. We will describe how the excellent biophysical properties of Centyrins make them ideal conjugation partners for applications designed to combine small molecule and large molecule opportunities.
Robert J. Hayes, Ph.D., Venture Leader and Vice-President, Janssen R&D, a Johnson & Johnson company

2:15
Case Study
Novel Pyrrolobenzodiazepine Payloads for ADC Therapies
The pyrrolobenzodiazepines (PBDs) are a family of naturally occurring antitumour antibiotics found in various Streptomyces species. Completely synthetic, highly potent PBD dimers have been developed as antitumour agents and these molecules have been modified to allow conjugation to tumour targeting antibodies. The resulting PBD antibody conjugates have exhibited excellent in vivo antitumour activity across a range of xenograft models.
Philip Howard, Ph.D., Chief Scientific Officer, MedImmune Spirogen Business Unit, United Kingdom

2:45
Unpublished Data
Antibody Drug Conjugates with Novel DNA Alkylating Agents: Design and Preclinical Evaluation
The cytotoxic effector molecule is a key component of antibody-drug conjugates (ADCs). A new class of potent DNA-alkylating agents, (IGNs), have been designed and synthesized for use in ADCs. These compounds are cytotoxic in vitro towards cancer cell lines, with IC50 values in the picomolar range. Results from preclinical evaluation of ADCs of these novel DNA alkylators will be presented.
Ravi J. Chari, Ph.D., Executive Director, Chemistry and Biochemistry, ImmunoGen, Inc.

3:15
Networking Refreshment Break in Poster & Exhibit Hall

4:00
Unpublished Data
DeBouganin: De-Immunized Cytotoxic Payload for Targeted Cancer Therapy
Immunotoxin fusion proteins represent a highly potent alternative to conventional anti-cancer agents. We have developed a de-immunized variant of the plant-derived, type I ribosome-inactivating protein (RIP), bouganin. Various antibody drug formats linked to deBouganin were engineered and characterized for biologic activity. The biologic characterization of deBouganin-conjugates as well as the Phase I clinical data are presented.
Glen C. MacDonald, Ph.D., Chief Scientific Officer, Viventia Bio Inc.

Towards Homogeneous ADCs - The Promise of Better Clinical Impact and Product Safety

4:30
Addressing Tumor Heterogeneity and Resistance; Production of Homogeneous ADCs with Combination Warheads
Homogeneous single species ADCs hold the promise to enhance the efficiency of tumor killing while reducing systemic damage and increasing their tolerability. Making many positional variants to assess the best candidate positions for conjugation is challenging using conventional cell based expression systems. Using biochemical protein synthesis methods, parallel production of many positional variants can be expressed in hours and rapidly assessed for function. We will describe the power and utility of the platform to address efficient non-natural amino acid incorporation and optimized conjugation kinetics for manufacturing. Finally we will demonstrate the design and manufacture of new classes of homogeneous mono- or multi-specific antigen-targeted antibodies conjugated to combinations of different warheads promising even better clinical impact and safety.
Trevor Hallum, Ph.D., Chief Scientific Officer, Sutro Biopharma, Inc.

5:00
Unpublished DataCase Study
Site Specific Bioconjugates - A Pathway to Better Biologics
Biological therapeutics are effective interventions in many diseases. However it is apparent that the natural protein is often not optimum due to shortcomings such as in potency PK, delivery or specificity. To address this, modifications or conjugations to the proteins/peptides have been made, for example to extend half-life, to incorporate cytotoxic moieties or to impart additional pharmacology. To do this well requires an exquisite understanding of the effect of the site of conjugation on the function, stability, pharmacology and toxicology of the resulting bioconjugate. The specific incorporation of a non-natural amino acid subsequently allows a detailed determination of how to build the optimal bioconjugate. We will discuss Ambrx's approach.
Peter A. Kiener, Ph.D., Chief Scientific Officer, Ambrx Inc.

5:30
Close of Day Two

5:30
Happy Hour @ Pier 39 Overlooking San Francisco Bay
This networking reception is at Players Sports Grill & Arcade, which has sweeping views of San Francisco Bay, and is just two blocks from the Hyatt. Enjoy buffet finger food and drinks (beer, wine, soft drinks) plus arcade games and pool tables. Advance RSVP is required when registering with an additional $125 fee.

Friday, June 6, 2014

7:30
Coffee

Track A

8:00
Chairman's Opening Remarks
Manuel Baca, Ph.D., Fellow, Antibody Discovery and Protein Engineering, MedImmune LLC

Library Design, Screening, Selection, and Display Technologies and Platforms

8:15
Unpublished Data
Effect of Library Design on Adnectin Properties
Adnectins against targets of therapeutic interest are selected from complex libraries based on the tenth human fibronectin type III domain. Libraries with higher sequence and structural diversity are expected to yield domains with higher affinity and poorer stability. We tested this assumption by evaluating 1,200 Adnectins from different libraries, and found critical elements of library design additional to overall diversity.
Daša Lipovšek, Senior Principal Scientist, Molecular Discovery Technologies, Bristol-Myers Squibb

8:45
Unpublished Data
Mammalian Cell Display Allows Co-Selection of Human Antibodies for Functionality and Developability
Mammalian cell display together with simultaneous secretion of IgG, allows antibodies to be selected for both functionality and excellent biophysical properties for development. Coupled with in vitro somatic hypermutation, this enables highly potent antibodies to be generated. The use of high-throughput sequencing during this process allows insight into maturation pathways, and can be used to rapidly identify optimized antibodies.
David J. King, Ph.D., Chief Scientific Officer, AnaptysBio

9:15
Unpublished DataCase Study
Micro-scale Developability Assessment in Discovery: Case Study with a ScFv Based Fifunctional
The presentation will outline a robust process we have established in the Discovery Research space to design, triage, and optimize biotherapeutic leads with optimal physicochemical properties before they reach the lengthy and costly Development phase.
Laura Lin, Ph.D., Director, Biophysics, Analytics, & Bioconjugation, Global Biotherapeutic Technologies, Pfizer Biotherapeutics Research

9:45
Networking Refreshment Break

10:15
Case Study
Selective Regulation of the Insulin Receptor by Human Allosteric Monoclonal Antibodies
Abstract not available at time of print.
Hassan Issafras, Ph.D., XOMA Corp.

10:45
Unpublished DataCase Study
The Better Biologic: Library Design Principles Inspired from Repertoire Systems Immunology
Synthetic antibody library technologies allow the creation and parallel selection of billions of engineered biologics. As even the largest libraries occupy only an infinitesimal subset of all theoretical sequence space, the choice of antibodies occupying a library can have a tremendous impact on the fitness of the library as a whole. High throughput sequencing of both natural repertoires and library selections have provided a powerful new method to directly observe the sequence activity landscape of antibody populations. In this presentation, I review some of the most relevant repertoire observations, and illustrate how they can be applied towards the design of a maximum diversity single domain library, and a pre-encoded general human affinity maturation landscape.
Jacob Glanville, Scientific Director, Distributed Bio

11:15
Unpublished DataCase Study
Using Stabilised Receptors as Antigens to Generate Therapeutic Antibodies to GPCR Targets
Stabilized receptors offer a breakthrough solution to the central challenge of reliably making pharmacologically active antibodies against GPCRs. They enable the production of purified, properly folded and functional protein when removed from the cell membrane for use as an antigen. This case study provides important validation of this solution and further demonstrates that StaR antigens preserve biologically relevant epitopes, thereby enabling generation of diverse panels of functional antibodies.
Catherine Hutchings, Ph.D., Principal Scientist, Antibody Discovery & Strategic Partnering, Heptares Therapeutics Ltd, United Kingdom

11:45
Unpublished Data
ReD - Ultrarapid Antibody Discovery Via Combined Cellular and Lambdoid Polyvalent Display
Retained Display (ReD), is a novel cytoplasmic display platform enabling rapid and seamless switching between cellular and lambdoid phage display. We report novel human germline antibody scaffolds that are fully soluble in the cytoplasm discovered using ReD and their use in a library built on the ReD platform.
Ben Kiefel, Ph.D., CEO and Co-Founder, Affinity BIO, Australia

12:15
Lunch on Your Own

1:25
Chairman's Remarks
Ted Randolph, Ph.D., Professor, Department of Chemical and Biological Engineering, University of Colorado, Boulder

Confront Aggregation Concerns in Early-Stage Development

Featured Presentation

1:30
Unpublished DataCase Study
Bernhardt Trout, Ph.D. Strategic Approaches for Understanding and Hindering Aggregation
Learn about a new strategic approach for developability based on applying both molecular and macroscopic modeling tools in order to gain an understanding of degradation processes with unprecedented detail and accuracy. Take an aggregation-themed focus on the Spatial-Aggregation Propensity and Developability Index algorithms, which can be applied from the discovery phase through the development phase to identify problems early on and address them. Also, similar tools for viscosity and crystallizability will be described. Note: The speaker will present remotely from Boston.
Bernhardt L. Trout, Director, Novartis-MIT Center for Continuous Manufacturing; Co-Chair, Singapore-MIT Alliance; Chemical and Pharmaceutical Manufacturing Professor, Department of Chemical Engineering, MIT

2:00
Case Study
Engineering Strategies to Cure Cellular Aggregation of a Difficult-to-Express Fusion Protein
Based on kinetic modeling of the cellular synthetic process, we compared different strategies (cell engineering, modulation of culture environment) to alleviate cellular aggregation and the associated poor expression of a recombinant Fc-fusion protein by CHO cells. Our analysis serves as a paradigm for multivariate optimization of DTE protein production.
David C. James, Ph.D., Department of Chemical and Biological Engineering, University of Sheffield, United Kingdom

2:30
Unpublished DataCase Study
High Throughput Developability Screening Methods Targeting Antibody Self/Cross Interaction
Developability issues, such as aggregation, low solubility, high viscosity and poor pK can be tracked to antibody self or cross interaction. High throughput methods are currently available to screen hundreds to thousands of antibodies within a single day to be compatible with early stage antibody discovery. A quick overview of a few high throughput self and cross interaction screening assays and their correlation. Depending on the progress of currently on-going mouse pK experiment, correlation of serum clearance with each individual assay will be discussed.
Yingda Xu, Ph.D., Group Leader, Protein Analytics, Adimab

3:00
Networking Refreshment Break

3:30
Unpublished Data
Aggregation in Biopharmaceuticals in Human Plasma and Serum: From In Vitro Analysis to In Vivo Implications
Aggregation phenomena can occur in vivo after the injection or infusion of a clear, non-aggregated protein solution. The aggregates formed at the injection site in tissue or in the bloodstream may have toxic and immunogenic effects. This talk presents new data on the characterization of the aggregates formed in vitro when different formulations of therapeutic proteins are mixed with human plasma and blood. Explore a model for the aggregation, and discuss clinical implications of the aggregation induced by biopharmaceuticals.
Tudor Arvinte, Ph.D., Professor, School of Pharmacy Geneva-Lausanne, University of Geneva, Switzerland and CEO, Therapeomic, Inc.

Approaches to Improve Prediction and Mitigate Risk of Immunogenicity

4:00
Unpublished DataCase Study
Clinical Relevance of Immunogenicity
This presentation will provide case study examples of how pre-clinical methods measuring drug induced T cell responses can be applied to select drugs with a reduced risk of clinical immunogenicity. Furthermore, new data will be presented on how aggregates in some formulations can trigger innate responses that ultimately enhance immunogenicity. The clinical relevance to these findings will be discussed.
Matthew Baker, Ph.D., Chief Scientific Officer and Director, Antitope, United Kingdom

4:30
Unpublished Data
Understanding the Immunogenicity Risk to Aggregated Particles in a Biotherapeutic
Protein aggregates in biotherapeutics, such fully human antibodies (mAbs), can be potentially immunogenic. You can encounter aggregated particles in formulations during the manufacturing, storage, and delivery process. The aggregate attributes that can play a role include protein sequence, particle size, and particle number. The immune status of the individual also modulates the response to such risk factors. During this talk, evaluate the threshold of immune response to the number and size of particles associated with aggregates and the relevance of the readout of in silico, in vitro, and in vivo assays in the context of a real-time formulation.
Vibha Jawa, Ph.D., Principal Scientist, Clinical Immunology, Amgen Inc.

5:00
Close of Conference

Track B

8:00
Chairman's Opening Remarks
Peter A. Kiener, Ph.D., Chief Scientific Officer, Ambrx

Alternatives to PEG for Plasma Half-Life Extension

8:15
Unpublished Data
PASylation - The Biological Alternative to PEGylation
Short plasma half-life is a major draw-back of most biopharmaceuticals. PEGylation of biological drugs is now widely applied, but has disadvantages with regard to high production cost and accumulation in various tissues. PASylation allows the simple genetic fusion (or chemical coupling) of a therapeutic protein or peptide with a voluminous hydrophilic and biodegradable polypeptide composed of Pro, Ala, and/or Ser to retard kidney filtration, thus allowing the design of better drugs with prolonged action.
Arne Skerra, Ph.D., Managing Director & Chief Scientific Officer, XL-protein GmbH, Germany

8:45
Unpublished Data
PK Modulation of Haptenylated Peptides Via Non-Covalent Antibody Complexation
Noncovalent antibody-peptide complexes can be applied to modulate peptide pharmacokinetics. Hapten-coupled peptide derivatives which activate the Y2R receptor were complexed with a hapten-binding antibody. Binding and signaling assays showed that modified peptides and peptide-antibody complexes retain better potency than PEGylated peptides. In vivo analyses of antibody-complexed peptides revealed improved serum half-life and weight reduction in a murine DIO model.
Ulrich Brinkmann, Ph.D., Expert Scientist, Roche Pharma Research and Early Development- Large Molecule Research, Roche, Germany

9:15
Unpublished Data
XTEN - A Biodegradable Alternative to PEG Enabling Biopharmaceuticals with Precisely Controlled Structure and Valency
Amunix has developed XTEN, a protein-based polymer that mimics the biophysical properties of PEG. XTEN is easily metabolized, thereby eliminating the risk of tissue accumulation. Single or multiple payloads can be conjugated or genetically fused to XTEN which allows the generation of monospecific, bispecific, as well as multivalent biopharmaceuticals. Examples of XTENylated biologics, including two clinical programs, will be discussed.
Volker Schellenberger, Ph.D., President and Chief Executive Officer, Amunix

9:45
Networking Refreshment Break

10:15
Albumin-Binding Adnectins as PK Enhancement Solutions
Adnectins are engineered proteins derived from human 10FNIII. Using mRNA display, we identified an Adnectin that binds to human and monkey serum albumin and exhibits enhanced in vivo pharmacokinetics vs. non-albumin-binding Adnectins. Clinical PK and immunogenicity data, mechanism of action, and the utility of albumin-binding Adnectins as PK enhancement solutions for therapeutic proteins will be presented.
Tracy Mitchell, Principal Scientist, Molecular Discovery Technologies, Bristol-Myers Squibb

Platform Technologies

10:45
Unpublished DataCase Study
Engineered Antibody Fragments Provide a Versatile Platform for Imaging Applications
The ability to engineer highly specific monoclonal antibodies into corresponding protein fragments provides a flexible platform to attach fluorescent and radioactive tracers for optical and PET imaging applications. Examples demonstrating the impact of different protein scaffolds, conjugation sites, clearance mechanisms, dosing levels and imaging schedules on the detection of immune cell and oncology targets will be presented.
Jean Gudas, Vice President, Research & Development, ImaginAb, Inc.

11:15
Unpublished DataCase Study
The Azymetric Platform: Novel Molecular Designs for Harnessing Novel Biological Activities
Azymetric™ is a robust bispecific antibody-engineering platform tailored for the design of novel therapeutic candidates with favorable developability features, altered valencies and specificities. Azymetric based molecular designs exhibit enhanced target decoration and retention, internalization, and effector activity. Supported by in vivo efficacy studies, the advantages of the platform for a number of lytic and ADC modalities will be discussed.
Surjit B. Dixit, Ph.D., Chief Technology Officer, Zymeworks Inc.

11:45
Spotlight Presentation to be Announced
For more information on spotlight presentations, please contact Patty Rose at (508) 614-1406 or prose@ibcusa.com

12:15
Lunch on Your Own

1:25
Chairman's Remarks
Arne Skerra, Ph.D., CSO, XL-protein GmbH, Germany

Targeting Strategies and Protein Delivery Approaches

Featured Presentation

1:30
Unpublished Data
Omid Farokhzad, M.D. Engineering of Polymeric Nanoparticles for Medical Applications
A variety of organic/inorganic materials are utilized to generate nanoparticles for drug delivery. Two most commonly used systems are polymeric nanoparticles and liposomes. Our goal is to review efforts in design and optimization of polymeric nanoparticles for medical applications, which formed the foundation for the clinical translation of the first-in-human targeted and controlled-release nanoparticles (BIND-014) for cancer therapy.
Omid Farokhzad, M.D., Associate Professor, Brigham and Women's Hospital & Harvard Medical School

2:00
Unpublished Data
Efficient Delivery of Biologics into Specific Cell Types Using the Endosome Escape Trap
The efficient delivery of biologics into the cell and out of the endosomes remains a key challenge in accessing the intracellular target landscape. Most conventional CPP's are not cell specific and the vast majority of their cargoes remain trapped within the endosomal compartment. The Endosome Escape Trap enables the specific capture of those rare classes of CPP's which deliver their cargoes to the cytoplasm. Data will be presented showing that certain CPP's from Phylomer libraries can effectively deliver their cargoes which require cytoplasmic delivery for their functional activity
Richard Hopkins, Ph.D., Chief Executive Officer, Phylogica Ltd., Australia

2:30
Unpublished Data
Targeted Delivery using Nanoparticles
Targeted nanotherapeutics provide an attractive alternative to traditional ADC's, in part due to their large size, multivalent display of targeting ligands, and considerable capacity for encapsulating small molecule drugs. Clinical translation of the first of these targeted nanoparticles has given rise to a new drug with a favorable toxicity profile, long circulating PK, and initial evidence of antitumor activity.
Daryl C. Drummond, Ph.D., Senior Director, Nanotherapeutics, Merrimack Pharmaceuticals

3:00
Networking Refreshment Break

3:30
Case Study
CDR-Restricted Engineering of Native Human scFvs Creates Highly Stable and Soluble Bi-functional Antibodies for Subcutaneous Delivery
In this study, we engineered a tetravalent scFv-Fc-scFv molecule, targeting two immunomodulatory targets, the soluble chemokine CXCL13, and a cell-surface inflammatory antigen. We demonstrated for the first time that, when native, human scFvs are aggressively optimized to func¬tion in that format, the high concentration formulation required for subcutaneous delivery of scFv-based bispecifics and low-fre-quency dosing is an achievable goal.
Brian Fennell, Ph.D., Principal Scientist and Research Group Leader, Global Biotherapeutics Technologies, Pfizer Inc.

4:00
Unpublished Data
Photo-Immunotherapy (PIT): A Unique Highly Cancer Cell-Specific Therapy Inducing Immediate Necrotic Cell Death Followed by Enhanced Nano-Drug Delivery and Immunological Response
Photo-immunotherapy (PIT) is a newly developed molecularly-targeted cancer photo-therapy, which is based on conjugating a near infrared photosensitizer, IR700, to monoclonal antibodies targeting cancer-specific cell-surface molecules. PIT damages cell membrane to induce rapid necrotic cell death, results in dramatically enhanced nano-particle delivery to cancer tissue and elicit host immunity, therefore, PIT can treat contaminating target-negative cancer cells and overcome inhomogeneity.
Hisataka Kobayashi, MD, Ph.D., Chief Scientist, Molecular Imaging Program, NCI/NIH

4:30
Screening for Antibodies that Target the Blood-Brain Barrier
The blood-brain barrier presents a substantial obstacle to brain drug delivery. To help address this issue, we have recently developed a variety of antibody screening and engineering tools specifically designed with the blood-brain barrier in mind. New screening paradigms and resultant antibodies that have preference for the brain vasculature will be discussed.
Eric V. Shusta, Ph.D., Professor, Chemical and Biological Engineering, University of Wisconsin-Madison

5:00
Close of Conference