2017 Archived Content

Analytical Characterisation of Biotherapeutics Track Banner


As more and more non-traditional and novel therapeutic concepts make their way down the development pathways, companies need to rethink and retool their analytical toolbox to address the myriad of complex challenges posed by these unique molecules. From developing new methods to evaluating the best technologies and approaches, CHI’s 4th annual Analytical Characterisation of Biotherapeutics invites scientists to showcase strategies to elucidate structure-function, determine glycosylation and higher order structure, characterise in vivo activity and assess biosimilarity.

Final Agenda

Recommended Short Course*

SC10: New Analytical Approaches & Strategies for Comparability & Biosimilarity

*Separate registration required

WEDNESDAY 15 NOVEMBER

07:45 Registration and Morning Coffee

COMPARABILITY & BIOSIMILARITY

08:30 Chairperson’s Remarks

Alistair Kippen, Ph.D., Vice President, Biologics Development, Ipsen

08:35 Preparation of a Strong and Convincing Biosimilar File Supported by Sophisticated Analytical Characterization

Martin_MuellerHans-Martin Mueller, Ph.D., Director, Bioprocess Development, Biologics & Vaccines, MSD

Demonstrating comparability for a commercial biosimilar product may present the greatest challenge of an analytical scientist’s career. This presentation will talk about the preparation of a robust analytical package for US and EU health authorities, in particular, how to be successful with demonstrating comparability through batch testing, extended characterization, stability studies and forced degradation.

09:05 QC Testing of Biopharmaceutical Higher Order Structure

Carl Jone, Ph.D., Senior Director, Head, Analytical Sciences Biologicals, UCB

Is biopharmaceutical Higher Order Structure (HOS) a critical quality attribute? If so, how do we monitor HOS in a QC environment? A case study will be presented on how native peptide mapping is being evaluated to determine if it is appropriate for a QC setting.

09:35 Approaches to Demonstrate Higher Order Structure Comparability of Biosimilars by HDX-MS

Christian_GrafChristian Graf, Ph.D., Scientist, Novartis BTDM-Technical Development Biosimilars, Novartis Pharma AG

Hydrogen/deuterium exchange mass spectrometry has become an important method to monitor conformational properties of biopharmaceuticals and is increasingly used for structure-function characterization and epitope mapping. Here we present capability and case studies for the use of HDX-MS in analytical comparability studies during biosimilar development.

10:05 MAM, It’s More than Peptide Mapping

David Lascoux, Business Development Manager, Waters Corporation

Peptide-centric monitoring of multiple product variants (Peptide map based MAM) has recently generated great interest and concerns. Currently, there is progression and validating of subunit mass based MAM methods for high throughput process monitoring and QC release assays. This seminar will discuss the benefits of applying a compliant ready LC/MS platform for effective deployment of both subunit mass and peptide map based MAM assays.


10:35 Coffee Break in the Exhibit Hall with Poster Viewing

CHARACTERISING COMPLEX BIOLOGICS

11:15 Analytical Characterization of Novel High Potency Toxin-Therapeutics

Daniel_HigaziDaniel Higazi, Ph.D., Director, Analytical Development, Biologics Development, Ipsen Biopharm

A detailed understanding of key structural features and degradation pathways is required to enable protein design and CMC development to proceed in a rational manner, whereby quality attributes are understood and appropriately controlled. Due to their highly potent nature, and resultant low dose, toxin-based therapeutics present some unique analytical challenges. Case studies will be presented where insight into quality attributes for toxin therapeutics has been gained using tailored analytical characterisation techniques.

11:45 Probing Protein Higher Order Structure with Mass Spectrometry

Viv_LindoVivian Lindo, Ph.D., Associate Director, Product Characterisation, MedImmune

  • Light scattering analyses
  • HDX-MS higher order structure determination
  • Protein folding and conformational dynamics
  • Characterisation of non-covalent interactions

12:15 High Resolution Methods to Evaluate Structure of Antibodies and Antibody-Antigen Complexes

Czeslaw_RadziejewskiCzeslaw Radziejewski, Ph.D., Senior Principal Research Scientist, Biophysical Chemistry, AbbVie Bioresearch Center

This presentation will focus on the application of transmission electron microscopy and other techniques to characterize biopharmaceuticals and will demonstrate power of such approaches to understand structure and solution behavior of antibodies and antibody-antigen complexes.

12:45 Development of Biotherapeutics: The Importance of Applying Orthogonal Analytics during Protein Stability Profiling

Natalia_MarkovaNatalia Markova, Ph.D., Principal Scientist - MicroCal BioScience, Malvern Panalytical

As the biopharmaceutical industry develops ever-more structurally complex molecules, there is a growing requirement for complementary analytics to ensure detailed and robust characterization profiles. Here, we’ll demonstrate two case studies where single-pass analytics proved insufficient in elucidating and understanding protein behavior at a molecular level. We’ll discuss small 2-domain recombinant protein contructs, and also biosimilar molecules, which both needed characterization using a variety of analytical technologies to reveal a complete picture of their stability profiles.


13:15 Luncheon Presentation: A Smart Microfluidic Technology for Early Discovery and Analytics

Anubhav_TripathiAnubhav Tripathi, Ph.D., Professor, Bioengineering and Medical Science, Brown University

Protein purity analysis by microfluidic separation offers distinct advantages over traditional capillary electrophoresis in sample consumption, ease of use, and speed of analysis. Using a smart microfluidic platform for high throughput quantitation and quality screening of proteins. The method utilizes a microchip which utilizes real-time electro-hydrodynamic optimization to eliminate variability in reported results, i.e. run-to-run and day-to-day variability, which may be caused by micro-scale fluctuations in the physical properties of chips, reagents, or instrument components.

13:45 Session Break

ASSESSING CQAs AND HIGHER-ORDER STRUCTURES

14:00 Chairperson’s Remarks

Hans-Martin Mueller, Ph.D., Director, Bioprocess Development, Biologics & Vaccines, MSD 

14:05 Tailoring Analytical Methods for the Assessment of Critical Quality Attributes of Antibodies

Christoph_RoesliChristoph Roesli, Ph.D., Analytical Project Leader, Biologics Technical Development and Manufacturing, Novartis Pharma AG

Distinct product-related variants originating from the manufacturing process or formed during storage have to be isolated or enriched to assess their bioactivity/potency and PK/PD. Here we present analytical strategies for the assessment of CQAs. Having tailored analytical methods and preparative tools to isolate or enrich product-related variants enables an early identification of CQAs. The CQA assessment is the starting point for a fit-for-purpose control strategy and subsequently a streamlined testing strategy.

14:35 Using Quantitative Proteomics to Link Critical Quality Attributes to Critical Process Parameters

Jonathan_BonesJonathan Bones, Ph.D., Principal Investigator, National Institute for Bioprocessing Research & Training (NIBRT), University College Dublin

Quantitative proteomics is a powerful tool to understand cellular behaviour at the molecular level. Quantitative proteomics of an IgG1 mAb producing CHO cell line was performed following systematic alteration of bioprocess conditions using a limited Plackett-Burman design of experiments approach. In addition to investigating changes in cellular behaviour, complete characterization of the expressed mAb was also performed to investigate the link between product critical quality attributes and alterations in critical process parameters.

15:05 QbD in Formulation Development - Advancements in the Use of High-Throughput Characterization and Strategies to Determine the Biorelevance of Critical Quality Attributes

Michael_SiedlerMichael Siedler, Ph.D., Head, NBE High-Throughput and Advanced Formulation Sciences, Drug Product Development, AbbVie Deutschland GmbH & Co KG

This talk will review how we are implementing QbD in formulation development of biologics by understanding the impact of formulation parameter on Critical Quality Attributes and their respective biorelevance. We will show examples of high throughput characterization methods and how they can de-risk challenges of novel molecule formats in early development. We will describe the use of predictive in vivo models to guide formulation development.

15:35 Refreshment Break in the Exhibit Hall with Poster Viewing

16:15 Quantitative LC MS in Biopharmaceutical Development – Case Studies from the Industry

Dan_Back_KristensenDan Bach Kristensen, Ph.D., Principal Scientist, Analytical Development, Symphogen

At Symphogen, quantitative LC MS is being used extensively during biopharmaceutical development for analysis of critical quality attributes, including chemical degradants (oxidation, deamidation, etc.), disulphide scrambling and glycan distribution. Here the technological platform is presented together with case studies from projects in preclinical and clinical development.

 16:45 Analytical Biosimilarity and Comparability – A Regulatory Perspective

Christina_VesselyChristina Vessely, Ph.D., Senior Consultant, Biologics Consulting

The focus of this discussion is on the regulatory expectations with respect to the establishment of biosimilarity or comparability. This includes a discussion on the selection of appropriate methods for release and extended characterization, as well as the development of protocols for the establishment of comparability or biosimilarity. Both activities require a thorough assessment of the biochemical, biological, and biophysical properties of the product in comparison with a reference material.

 

17:15 Problem-Solving Breakout Discussions (View All Breakout Discussions)

Multi-Attribute Monitoring by Mass Spectrometry versus Separate HPLC-Based Methods for Release Testing

Christoph Roesli, Ph.D., Analytical Project Leader, Biological Technical Development and Manufacturing, Novartis Pharma AG

  • Fact 1: Multi-attribute monitoring (MAM) by MS is state-of-the-art during product development / characterization
  • Fact 2: Release testing is (almost) exclusively based  on HPLC methods
  • Kick-starter 1: Is MAM by MS for future release testing strategies required?
  • Kick-starter 2: How to bring MAM by MS to release testing?
  • Kick-starter 3: MAM is information-rich. How to deal with these information for release?

Experience/ Lessons Learned with Introducing Lab Automation in Drug Product Development

Michael Siedler, Ph.D., Head, NBE High-Throughput and Advanced Formulation Sciences, Drug Product Development, AbbVie Deutschland GmbH & Co KG

  • Experience in setting up workflows and converting analytical methods into HT format
  • Hurdles and solutions around the required IT infrastructure
  • Experience with applying advanced data science tools such as predictive analytics & machine learning algorithms

New Approaches in Biologics Discovery

Moderator: Alexey Rak, Ph.D., Head, Biostructures and Biophysics, Integrated Drug Discovery, Sanofi R&D

  • Predict developability
  • Predict deviceabilty
  • Low material consumption and high throughput methods for biologics characterization

 

18:15 Networking Reception in the Exhibit Hall with Poster Viewing

19:15 End of Day

THURSDAY 16 NOVEMBER

08:00 Registration and Morning Coffee

TECHNOLOGIES & APPROACHES TO IMPROVE CHARACTERISATION - COMPARE & CONTRAST

08:30 Chairperson’s Remarks

Michael Siedler, Ph.D., Head, NBE High-Throughput and Advanced Formulation Sciences, Drug Product Development, AbbVie Deutschland GmbH & Co KG


08:35 KEYNOTE PRESENTATION: Leveraging the Multi-Attribute Method (MAM) to Improve Biotherapeutic Characterization

Richard RogersRichard Rogers, Ph.D., Scientist 4, Just Biotherapeutics

Characterization of complex biotherapeutics using highly resolving mass spectrometry has resulted in a better understanding of the post-translational modifications that are crucial for safety and efficacy. These modifications are used to guide the manufacturing process and the release strategy for biotherapeutics. We have developed and implemented a mass spectrometry-based multi-attribute method (MAM) that monitors known modifications but also has the ability to identify new modifications on the biotherapeutics.

09:05 Poster Highlights:

Poster Highlight I: Site-Specific O-Glycan Analysis Using a Novel O-Glycan Protease and LC-MS/MS

Maria Nordgren, MSc., Senior Scientist, Application Development & Support, Genovis AB

Characterization of O-glycosylated proteins have suffered from a lack of specific enzymes and new tools have been needed. This work presents analytical workflows for site-specific O-glycan characterization of proteins using a new O-glycan specific protease. The enzyme, discovered in Akkermansia muciniphila, binds specifically to O-glycans on native glycoproteins and digests the peptide backbone N-terminally of S and T residues. As an example, O-glycopeptides of Etanercept, a Fc-fusion protein with an O-glycosylated hinge region, has been characterized using LC-MS/MS.

Poster Highlight II: Monitoring of Non-Human Glycan Epitope on Biotherapeutic Glycoproteins with Advanced MS Technologies

Myung Jin Oh, Ph.D., Research Professor, Graduate School of Analytical Science and Technology (GRAST), Chungnam National University & Asia-Pacific Glycomics Reference Site

Therapeutic glycoproteins represent a great accomplishment for treatment of various diseases. Biotherapeutics are frequently manufactured in mammalian expression systems to achieve appropriate glycosylation, and the glycosylation pattern is often critical for the drug's stabilty, immunogenicity, PK/PD and bioactivity. Analysis of the non-human glycan is critical to regulate of potential immunogenicity for process development and manufacturing procedures of therapeutic glycoproteins. Here, we propose LC/MS and MS/MS screening as a method for rapid identification and structural elucidation of biopharmaceutical glycosylation containing non-human glycan epitope.

Poster Highlight III: Application of Artificial Neural Networks in the Development of Protein Formulation

Lorenzo Gentiluomo, MSc., PhD Student, R&D (Pharmacy), Ludwig-Maximilians-University Munich

The goal of the EU-ITN PIPPI Project is to provide a database of proteins which provides in depth insight into important protein properties that govern colloidal and conformational protein stability in order to direct successful protein formulation development. Artificial Neural Networks (ANNs) represent a promising modeling technique for this data set with non-linear relationships. ANNs models were applied successfully to predict a series of important protein stability indicator.

09:35 SEC-MS for Characterization of Product-Related Impurities of Monoclonal Antibody

Li_ZangLi Zang, Ph.D., Associate Director, Analytical Development, Biogen

Case studies will be shared for applying an SEC-MS method to characterization of high-molecular weight and low-molecular weight species in monoclonal antibody biotherapeutics.


10:05 Pyrogen Detection by Monocyte Activation Test in Antibody Formulations

Roger_GrauRoger Grau, Ph.D., Head, Research & Development, BU Confarma, Solvias AG

Detection of pyrogens - fever inducing substances - relies predominantly on the rabbit pyrogen test. In preparations where endotoxin is the only potential contaminant, the rabbit test can be replaced by a specific endotoxin test. The Monocyte Activation Test provides a sensitive, reliable alternative for those cases, where potential contaminants other than endotoxin might be present. It monitors the release of cytokines induced by pyrogens present in the sample using human cells as test system.

10:35 Coffee Break in the Exhibit Hall with Poster Viewing

11:15 Screening for Potent T-Cell Dependent Bispecific Antibodies for Inducing Cytotoxicity of Tumor Cells Using an Impedance-Based Assay Platform

Elaine_MaiElaine Mai, MSc, Senior Scientific Researcher, Biochemical and Cellular Pharmacology, Genentech, Inc.

Compared with IncuCyte assay using caspase-3/7 readout, the impedance-based assay is more sensitive in detecting killing of low target expressing cells. Also, the impedance assay has a similar potency ranking for different TDB clones to the cell titer glo assay. In addition, the assay generated similar EC50s to FACS using propidium iodide staining. In conclusion, the impedance platform is superior to the other assay methods in supporting TDB candidate selection with the advantages of being label free and having better sensitivity.

11:45 Integrating Novel Tools into Development Workflow of Biologics: nanoDSF and MST for Discovery, Development and QC

Alexey_RakAlexey Rak, Ph.D., Head, Biostructure and Biophysics, Integrated Drug Discovery, Sanofi R&D

Modern drug discovery operations require characterization of biomolecular interactions to be both time- and cost-effective as well as to be highly precise and reproducible. Here we report applications of two novel methods, nano-Differential Scanning Fluorimetry (nanoDSF) and MicroScale Thermophoresis (MST), that we are applying in our biologics discovery and characterization operations. The examples of the demonstrated effectiveness of the nanoDSF and MST will be presented and discussed.

GE Healthcare_new12:15 Luncheon Presentation: Development of Key Characteristics of Biopharmaceuticals Accelerated using SPR

Åsa Frostell, Senior Scientist, Purification and Analysis, GE Healthcare Life Sciences

Reliable analytical tools are important for economical process development, production and batch release of therapeutic antibodies and new emerging drug formats. This presentation will discuss the benefits that surface plasmon resonance (SPR) technology brings to the development process, taking into account regulatory expectations. In particular, accelerating effective antibody drug conjugate (ADC) design, increasing obtained information regarding relative potency, and examples of simplified analyses of FcRn and Fcγ receptor binding will be presented.

13:00 Dessert Break in the Exhibit Hall with Poster Viewing

13:30 End of Analytical Characterisation of Biotherapeutics