SC2/SC6: Translational Biotherapeutic Development Strategies Part I: Discovery, Molecular Assessment and Early Stage Development

 

Part 1: SUNDAY, August 30 | 10:00 am - 1:00 PM

PART 1 (SC2): Translational Biotherapeutic Development Strategies: Discovery, Molecular Assessment and Early Stage Development 10:00 AM – 1:00 PM
PART 2 (SC6): Translational Biotherapeutic Development Strategies: Analytical and Clinical Considerations  2:30 – 5:30 PM

COURSE AGENDA:

Part 1: Discovery, Molecular Assessment and Early Stage Development

The rapid rise of antibody-based therapies is due to their desirable safety profile, target specificity, and efficacy. Sources for antibody leads include immunization of animal species, phage-displayed antibody libraries, and direct cloning of antibody encoding genes from plasma and memory B cells of animals and humans. Antibody therapies come in different forms and sizes, including naked IgGs, ADCs, bispecific antibodies, Fc fusion proteins, radioimmunoglobulins, and antibody fragments. Each modality requires an array of complex engineering steps such as humanization, affinity maturation, Fc-engineering, and linker chemistry. Part 1 of the course will discuss the latest progress in antibody sources, protein engineering, and drug target selection.

10:00 Introduction

Zhiqiang An, PhD, Professor, Chemistry; Director, Texas Therapeutics Institute, University of Texas Health Science Center at Houston

10: 15 Sources of Antibodies and Antibody Drug Modalities: ADC, Bispecific, Naked Antibody, CAR-T

Zhiqiang An, PhD, Professor, Chemistry; Director, Texas Therapeutics Institute, University of Texas Health Science Center at Houston

Naked mAbs are still the dominant modality for therapeutic antibodies. However, advanced antibody drug modalities, such as antibody drug conjugates (ADCs), bispecific antibodies, and chimeric antigen receptor (CAR)-T constructs, are rapidly emerging. This lecture will discuss: 1) antibody drug sources from hybdridomas, phage-displayed antibody libraries, and single plasma or memory B cells; and 2) generation of mabs in advanced antibody drug modalities such as ADCs, bispecific antibodies and CAR-T constructs.

11:15 Refreshment Break

11:45 Considerations for Target Selection, Antibody Preclinical Screening & Development

Gadi Bornstein, PhD, Senior Director, Biologics Discovery, TESARO, Inc.

The main objective of this short course is to provide a comprehensive overview of key preclinical considerations for developing antibody therapeutics. This course will cover the antibody discovery process, antibody modes of action, as well as considerations for target selection and validation. An overview of antibody platforms and screening strategies for candidate selection will also be described. In addition, considerations for selecting the optimal animal model(s) to enable translation to the clinic will be discussed. Finally, examples of FDA-approved therapeutic antibodies will be provided.

12:45 Discussion and Questions

1:00 Close of Part 1

Part 2: SUNDAY, August 30 | 2:30 - 5:30 PM

Part 2: Analytical and Clinical Considerations

Unlike small-molecule drugs, therapeutic antibodies are large, complex molecules that are not easily formulated or delivered, and they are produced as heterogeneous mixtures of molecules including different glycoforms that can vary greatly in molecular structure. In designing antibody therapeutics, it is sometimes desirable to diminish or abolish the ADCC and CDC functions while retaining its pharmacokinetic profile, in the case of a “benign blocker” antibody. As a result, complex analytical tools have been developed and optimized for the molecular and functional characterization of antibody therapeutics. Part 2 of the course will discuss the protocols for antibody affinity and biophysical characterization, assessment of Fc-immune effector function, and pharmacokinetics of mAbs and Fc-fusion proteins.

2:30 Introduction

Zhiqiang An, PhD, Professor, Chemistry; Director, Texas Therapeutics Institute, University of Texas Health Science Center at Houston

2:45 Discovery and Optimization of Antibodies for Therapeutic Settings

Juan Carlos Almagro, PhD, Founder and CEO, GlobalBio, Inc.

This presentation will provide an overview of the FDA-approved therapeutic antibodies, with emphasis on the methods used for their discovery and optimization. Case studies of antibody humanization will be discussed. Also, a comparison of the antibody phage display libraries published in the last decade will be presented. These libraries represent the state of the art in the discovery and development of therapeutic antibodies via phage display. The comparison will be focused on the quality of the libraries, types of antibody repertoires used as substrates to build the libraries, their performance in terms of the number of positive clones per panning, hit rate, affinity, and developability of the selected antibodies.

 

3:45 Refreshment Break

4:15 Assessment of Fc Effector Functions of Therapeutic Antibody Candidates

An Song, PhD, Chief Scientific Officer, Immune-Onc Therapeutics, Inc.

Therapeutic antibodies rely on two types of functionalities to achieve clinical efficacy: target-specific binding by the Fab domain and immune-mediated effector functions via interaction of the Fc domain with receptors on various cell types. It is important to understand the role of Fc-mediated functions in mechanisms of action, efficacy and safety. This talk will cover current strategies and technologies in assessing Fc functionality of candidate therapeutic antibodies and Fc-containing proteins.

5:15 Discussion and Questions

5:30 Close of Short Course

INSTRUCTOR BIOGRAPHIES:

Almagro_Juan_CarlosJuan Carlos Almagro, PhD, Founder and CEO, GlobalBio, Inc.

Dr. Juan C. Almagro is an internationally recognized expert in engineering and development of antibody-based therapeutics. In part with support from the National Science Foundation, he founded GlobalBio to provide collaborative services in the areas of discovery, optimization and development of biotherapeutics. Prior to founding GlobalBio, he was a Senior Director at Pfizer and Research Fellow and Head of Antibody Design at Johnson and Johnson. Before joining the Pharma/Biotech industry, Dr. Almagro was Visiting Scientist at Florida International University, Affiliated Visiting Scientist at Fred Hutchinson Cancer Research Center, Visiting Professor at Simon Fraser University and Associate Professor and Group Leader at The National University of Mexico. He has authored over 70 publications, encompassing more than 50 peer-reviewed scientific articles, 6 book chapters, and 20 international patents. Dr. Almagro serves as reviewer in Immunology and Protein Engineering journals, as well as for grant agencies in several countries. He has participated in the Scientific Advisory Boards of several Biotech companies, has chaired and given talks and lectures at major domestic and international scientific meetings, and has been expert witness in several Intellectual Property litigations between large biopharma organizations.

An_ZhiqiangZhiqiang An, PhD, Professor, Chemistry; Director, Texas Therapeutics Institute, University of Texas Health Science Center at Houston

Dr. Zhiqiang An is Professor of Molecular Medicine, the Robert A. Welch Distinguished University Chair in Chemistry, and Director of the Texas Therapeutics Institute at the University of Texas Health Science Center at Houston. His laboratory focuses on cancer antibody drug resistance mechanisms, biomarkers for cancer therapeutic antibodies, and antibody drug discovery targeting cancer and infectious diseases. Dr. An also directs the Therapeutic Monoclonal Antibody Lead Optimization and Development Core Facility funded by the Cancer Prevention and Research Institute of Texas (CPRIT). Previously, he served as Chief Scientific Officer at Epitomics, Inc. and was Director of Biologics Research at Merck Research Laboratories. He started his biotech career at Millennium Pharmaceuticals. Dr. An received his Ph.D. degree from the University of Kentucky and his postdoctoral training at the University of Wisconsin-Madison. He is an elected fellow of Society for Industrial Microbiology and Biotechnology. He is also an elected fellow of the American Academy of Microbiology.

Bornstein_GadiGadi Bornstein, PhD, Senior Director, Biologics Discovery, TESARO, Inc.

Dr. Bornstein has twenty years of experience in Oncology R&D with an emphasis in preclinical antibody discovery and development. Dr. Bornstein currently leads biologics discovery efforts at TESARO, a GSK company. He received his B.S. in biochemistry at the University of California, Davis and his doctoral degree in biochemistry at the University of Southern California Keck School of Medicine. Dr. Bornstein completed his postdoctoral training at Stanford University in the Division of Immunology and Rheumatology.

Following his postdoctoral training, Dr. Bornstein joined Amgen Fremont, Inc. (formerly Abgenix, Inc.) as a Staff Scientist in the Preclinical Oncology department. Dr. Bornstein has held roles of increasing responsibility at AstraZeneca, Pfizer, and Novartis, where he was a project team leader, lead biologist, and key contributor to scientific strategies for multiple oncology programs.

Song_AnAn Song, PhD, Chief Scientific Officer, Immune-Onc Therapeutics, Inc.

An Song, Ph.D, is Senior Vice President of Development Sciences at Immune-Onc Therapeutics, Inc., accountable for translational development of Immune-Onc’s portfolio, including preclinical PKPD and toxicology evaluation, clinical pharmacology, bioanalytical and biomarker/diagnostic development and certain analytical aspects of technical development. Prior to Immune-Onc, An was a Senior Director in BioAnalytical Sciences at Genentech, where she led the Assay Development and Technology group for the company’s large molecule portfolio globally. During her 16-year tenure at Genentech, An contributed to, and oversaw 40+ IND/CTA and BLA/MAA regulatory filings for products including Rituxan@, Avastin®, Herceptin®, Lucentis ®, Kadcyla®, and Tecentriq®. Additionally, she played a significant role for the development and approval of Ocrevus®.

An holds a B.S. in Biochemistry from Nanjing University in China. She received her PhD. in Biochemistry & Molecular Biology from Indiana University and completed a postdoctoral fellowship in immunology at Stanford University. Upon completion of postdoctoral work in T-cell activation she joined Stanford as a Research Assistant Professor and as faculty of the Immunology Program. An has published a number of original manuscripts, review articles and book chapters, as well as contributed to several industry white papers on immunogenicity and antibody Fc effector function evaluation. She is an active member of American Association of Pharmaceutical Scientist (AAPS), having served as an executive member of the Biotech Section and the chair of Therapeutic Product Immunogenicity (TPI) Focus Group/Community.


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