Cambridge Healthtech Institute’s Sixth Annual
High-Concentration Protein Formulations:
Analytics, High Viscosity, Aggregation, Devices and Delivery
Part of CHI's Ninth Annual The Bioprocessing Summit

August 23-24, 2017 | Westin Copley Place | Boston, MA


At higher concentrations, proteins or antibodies exhibit characteristic problems including aggregation, precipitation, gelation, and increased viscosity. Development of these high-concentration protein formulations results in several manufacturing, stability, analytical, and delivery challenges. The popular High-Concentration Protein Formulations conference will feature informative, high quality case studies and successful strategies to overcome the problems you are facing with development and delivery of high-concentration protein formulations.

Final Agenda

Wednesday, August 23

7:00 am Registration Open and Morning Coffee

PROTEIN-PROTEIN INTERACTIONS, AGGREGATION & FORMULATION DEVELOPMENT

8:05 Chairperson’s Opening Remarks

Tom Laue, Ph.D., Professor Emeritus, Biochemistry, University of New Hampshire

8:15 KEYNOTE PRESENTATION: Considerations of Protein Solubility for High Concentration Formulation Development

Jifeng Zhang, Ph.D., Senior Director, Global Head of Device-ability, Global Pharmaceutical Development Biologics, Sanofi

Low protein solubility and high viscosity of solution are some of the major challenges in development, manufacturing and delivery of high concentration protein formulation. In this presentation, we will discuss various considerations and strategies to overcome the protein solubility issue for high concentration protein formulation development.

9:00 Probing Complex Protein-Protein Interactions at High Concentrations

Tom_LaueTom Laue, Ph.D., Professor Emeritus, Biochemistry, University of New Hampshire

There are several methods for detecting and characterizing high-concentration, protein-protein interactions when there is only one protein component. However, high-concentration formulations may contain several components and species. Furthermore, high-concentration formulations will be introduced into complex, concentrated solutions, such as serum. Fluorescence-detected analytical ultracentrifugation (AU-FDS) provides a first-principle method for characterizing the behavior of a single component in a complex mixture. Insights provided by AU-FDS for both single-component formulations and serum will be presented and discussed.

9:30 Predicting High-Concentration Behavior from Low-Concentration Data: Need for Caution

Atul_SalujaAtul Saluja, Ph.D., Associate Director, Global Pharmaceutical Development Biologics, Sanofi

Prediction of aggregation behavior (rates or trends per se) many times becomes necessary either as a function of temperature or protein concentration. Such approaches routinely rely on linear analysis wherein trends at lower protein concentration are projected to hold at higher protein concentrations. In this talk, data will be presented to emphasize the need for caution in employing such a linear predictive approach. Potential pitfalls in predicting optimal formulation conditions for concentrated solutions from dilute solution data will also be highlighted.

Rockland 10:00 Coffee Break in the Exhibit Hall with Poster Viewing

10:45 Innovative Approaches to Achieving Stable High-Concentration Protein Compositions

Jan_JezekJan Jezek, Ph.D., CSO, Research & Development, Arecor, Ltd.

The need to develop stable, low-viscosity formulations of therapeutic proteins is greater than ever, and new approaches to formulation are needed to overcome associated stability and viscosity challenges. The talk will describe several novel compositions of concentrated proteins allowing development of liquid high-concentration protein products with superior stability profiles, with a focus on the control of aggregation as well as other quality attributes such as viscosity and fragmentation.

11:15 PANEL DISCUSSION: Opportunities and Challenges in Adoption and Implementation of Disruptive Technologies for High-Concentration Protein Formulations

Moderator:

Tom Laue, Ph.D., Professor Emeritus, Biochemistry, University of New Hampshire

Panelists:

Atul Saluja, Ph.D., Associate Director, Global Pharmaceutical Development Biologics, Sanofi

Jan Jezek, Ph.D., CSO, Research & Development, Arecor, Ltd.

Jifeng Zhang, Ph.D., Senior Director, Global Head of Device-ability, Global Pharmaceutical Development Biologics, Sanofi

Michael S. Marlow, Ph.D., Senior Staff Scientist, Protein Biochemistry, Regeneron Pharmaceuticals, Inc.

Lindy Biosciences 11:45 Particle Engineering Platform for High-Concentration Protein Suspensions  

Deborah_BitterfieldDeborah Bitterfield, Ph.D., CEO and Founder, Lindy Biosciences, LLC

Suspension formulations can alleviate the viscosity and stability challenges associated with subcutaneous delivery of biologics. We will present a novel dehydration technology, Microglassification, which combines the stability of solid formulations with particle-engineering expertise. The resulting dense protein particles are ideal for high-concentration, injectable suspensions.

12:15 pm Luncheon Presentation (Sponsorship Opportunity Available) or Enjoy Lunch on Your Own

1:00 Session Break

PROCESS AND MANUFACTURING CONSIDERATIONS FOR HIGH CONCENTRATION FORMULATIONS

1:45 Chairperson’s Remarks

Jan Jezek, Ph.D., CSO, Research & Development, Arecor, Ltd.

1:50 FEATURED PRESENTATION: Mechanistic Investigation on Grinding-Induced Subvisible Particle Formation during Mixing and Filling of Monoclonal Antibody Formulations

Yuh-Fun_MaaYuh-Fun Maa, Ph.D., Senior Principal Engineer, Pharmaceutical Processing & Technology Development, Genentech, Inc. - A Member of the Roche Group

Monoclonal antibody (mAb) particle formation observed during bottom mounted mixing and filling by piston pump was investigated to understand the root-cause mechanisms leading to subvisible particle formation. The design of the mixer and the pump plays a critical role and any designs with contacting moving parts may grind the mAb molecules to immediately form subvisible particles. Stress types associated with grinding action have been assessed in various stress models.

2:20 Formulation and Process Strategies to Improve TFF Performance

Steven_GengSteven Geng, Ph.D., Research Scientist, Bioproduct Pharma Design, Eli Lilly and Company

Desire for higher doses of biologics has driven a need to formulate at higher concentrations. Tangential flow filtration (TFF) is a commonly used unit operation to concentrate protein. Here we have identified and studied how to overcome factors that limit TFF performance.

2:50 Upstream/Downstream Processing Impact on High-Concentration Formulation Stability: A Case Study

Steve Lantz, Scientist I, Protein Pharmaceutical Development, Biogen

Changes to cell culture and purification processes impacted the aggregation stability of a high-concentration mAb formulation. This case study details the process controls established to maintain product quality and how formulation optimization inhibited aggregation related to certain chemical modifications.

3:20 Use of First-Principles to Guide Process Development for High Concentration Protein Drug Product

Zhao Yu, Ph.D., Associate Senior Consultant Engineer, Bioproduct Research and Development, Eli Lilly and Company

High concentration protein drug products often have higher viscosity and density, which may result in challenges in process development and manufacturing. This talk presents a case study where engineering principles and computational fluid dynamics modeling were used to achieve mechanistic understanding of the controlling parameters in a mixing operation. They also guided the design of experiments using surrogate fluids or drug product, which gave further validation of the process knowledge and provided scale-up rationale.

3:50 Refreshment Break in the Exhibit Hall with Poster Viewing

4:45 PLENARY KEYNOTE PRESENTATION

6:00 Networking Reception in the Exhibit Hall with Poster Viewing

7:00 Close of Day

Thursday, August 24

8:00 am Registration Open and Morning Coffee

RAPID EXCIPIENT SCREENING

8:25 Chairperson’s Remarks

Atul Saluja, Ph.D., Associate Director, Global Pharmaceutical Development Biologics, Sanofi

8:30 Screening Formulation Conditions with High Concentration Self-Interaction Nanoparticle Spectroscopy (HC-SINS)

Michael_MarlowMichael S. Marlow, Ph.D., Senior Staff Scientist, Protein Biochemistry, Regeneron Pharmaceuticals, Inc.

Manufacturing and dosing of therapeutic monoclonal antibodies frequently call for high protein concentration solutions and the non-ideality that follows complicates reliable extrapolation of critical properties from measurements made under dilute conditions. This talk will illustrate the utility of a novel implementation of SINS in bridging the dilute-high concentration gap by assessing the concentration dependence of protein-protein interactions and the effect various formulation strategies have on colloidal behavior.

9:00 Preferential Interactions of Formulation Excipients with High-Concentration IgG1 Monoclonal Antibody Solutions

Chaitanya_SurdrikChaitanya Sudrik, Postdoctoral Associate, Chemical Engineering, Massachusetts Institute of Technology

The aggregation and viscosity behavior of high concentration mAb formulations is impacted by the addition of weakly interacting excipients. Here, we present the data for the preferential interaction of commonly used excipients like trehalose, L-arginine HCl and sodium chloride with three therapeutically relevant IgG1 antibody molecules. We also present data for the impact of excipient addition on protein stability and derive further insight on the underlying molecular mechanisms.

9:30Selected Poster Presentation: A Modeling Approach For Excipient Selection in High-Concentration Protein Formulations

Christoph Brandenbusch, Ph.D., Group Leader, Department of Biochemical and Chemical Engineering, Laboratory of Thermodynamics, Technical Univ. of Dortmund

HCPFs are commonly achieved by addition of suitable FDA approved excipients (e.g. salts, sugars, amino acids, surfactants) to aqueous protein solution based on heuristic approaches/decisions. This approach does not account for negative influences induced by the excipients (e.g. agglomeration) in early stage development. In this work, we present first results on a novel method to identify suitable excipients/excipient combinations based on their intermolecular interactions with the protein in solution.

10:00 Coffee Break in the Exhibit Hall with Poster Viewing

10:45 Pre-Formulation Approaches to Understand Instabilities in Protein Solution

Ashlesha_RautAshlesha S. Raut, Ph.D., Senior Scientist, Biologics and Vaccine Formulation, Merck

The aim of formulation development of protein therapeutics is to produce efficacious products wherein the protein remains in the solution and maintains stability across its shelf life. With the ever-growing biologics pipeline, continual efforts are directed towards the implementation of high throughput approaches to select robust candidate and formulation. This presentation discusses the impact of formulation and key process parameters on the protein stabilities and formulation selection strategies in the early stages of development.

VISCOSITY, INJECTABILITY AND DELIVERY

11:15 High Concentration Relative to What? Some Case Studies

Zahra Shahrokh, Ph.D., CMC Consultant and Chief Development Officer, STC Biologics

For each protein, a high concentration is a relative term, where even 10 mg/ml might be a challenge, for example for a non-Mab entity, and achieving 10x higher concentration requires scientific and empirical development approaches. Meeting the toxicology delivery requirements of protein therapeutics can sometimes be a higher hurdle than the clinical program in terms of product concentration and compositions. This talk with provide case examples of different types of proteins and delivery routes that necessitated creative approaches to formulation design.

11:45 Challenges of High Protein Concentration Formulations for Ocular Drug Delivery

Meike_IrngartingerMeike Irngartinger, Ph.D., Senior Scientist, Early Stage Pharmaceutical and Process Development, F. Hoffmann-La Roche Ltd.

Formulation development for ocular drug delivery is a highly challenging area when it must deal with high concentrations aiming on less frequent dosing schemes. Results of a case study on high concentration formulation development for ocular application will be presented. Further on, the challenge of high concentration combined with low fill volume on drug product manufacturing and administration is discussed.

12:15 pm Enjoy Lunch on Your Own

1:15 Dessert Refreshment Break in the Exhibit Hall and Last Chance for Poster Viewing

1:55 Close of Conference