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Day One
Thursday, January 15
7:00am – 3:00pm Registration Open
7:30 Morning Coffee
 8:15 Chairperson’s Opening Remarks
Palani Palaniappan, Ph.D., Senior Director, Pharmaceutical Sciences,
Millennium Pharmaceuticals, a Takeda Oncology Company
PREFORMULATON AND
EARLY CHARACTERIZATION
 8:25 The Discovery-Development Interface, an Important Relationship in Successful Dosage Form Design for Biotherapeutics
Kevin King, Ph.D., Director, Formulation Development and Product Enhancements, Global Biologics, Pfizer
The Discovery-Development interface is key to ensure a pipeline that contains well tolerated, safe, efficacious and convenient dosage forms for biotherapeutics. Early experiments based upon theoretical hot spot screening and purposeful degradation identify any formulation challenges to be addressed as potent molecules are progressed in to development. This presentation will provide an overview of approaches that can aid molecule selection from a formulation perspective and highlights the importance of early formulation charaterisation application for effective formulation and process design.
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The benefits of an effective Discovery-Development interface
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How early formulation characterization tools are applied to aid molecule selection
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Use of purposeful degradation studies
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The application of early pharmaceutics screening learnings to formulation development
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Formulation strategy options
9:05 Current Trends in Biologics Formulations: Development in Oncology versus Inflammation, New Development Tools, and Convenience Devices
Palani Palaniappan, Ph.D., Senior Director, Pharmaceutical Sciences, Millennium Pharmaceuticals, a Takeda Oncology Company
Biologics development in non oncology areas during the past several years has enabled significant advances in terms of product formats, drug product development approaches, patient convenience devices and regulatory approaches. More recently, several biologics are being developed in oncology indications, where many of the above non oncology requirements and approaches must be balanced with the need to have the products launched sooner in potentially unmet medical needs. A general overview will be presented with some specific examples of drug product development approaches and opportunities.
 9:35
Using Forced Degradation Techniques: A case study using temperature and agitation-induced stress to identify and optimize a liquid drug product formulation for an IgG1 monoclonal antibody
Eva Kras, B.S. in Pharmacology, Research Associate III, Analytical Biochemistry and Formulations, Seattle Genetics
Monoclonal antibodies (mAbs), an emerging class of protein-based drugs, require the development of stable and robust liquid drug product formulations. Three lead formulation candidates, identified from a frozen bulk drug substance stability study, were employed to screen a variety of pharmaceutically acceptable excipients in order to identify and optimize a stable liquid drug product formulation. By utilizing forced degradation techniques, such as temperature and agitation-induced aggregation, material requirements, timelines and resources were minimized without compromising the stability of the formulation.
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This presentation will demonstrate the ability to identify a robust and stable liquid drug product formulation using minimal material, resources, and overall evaluation time
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The audience will gain a perspective on how useful this approach was for developing a stable DP formulation in a short time frame with minimal resources
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They will also see that is forced degradation can be correlated to real time data
10:05 Coffee Break in the Exhibit Hall
FORMULATION COMPOSITION SCREENING AND
OPTIMIZATION
 11:00 High-Throughput Analytics Lab (HTL) for the Market Formulation Development of Antibodies
Kurt Forrer, Ph.D., Senior Fellow, Novartis Pharma AG
A concept will be presented how several hundreds of formulations can be prepared by a robot system and the corresponding solutions can be analyzed. It is possible to measure the aggregates, the oxidized and deamidation variants, the content, the fragments, the charge variants plus the by- and degradation products in a high-throughput mode. To find out the most stable formulations a stability study in microtiterplates will be run and afterwards analyzed again. A concept will be shown how the huge amount of data can be evaluated. Attendees will learn what can be possible with a robot system in terms of preparation of formulations and analytical characterization in a high-throughput mode. They get familiar how a huge amount of data can be interpreted in a quick way.
 11:30 Development of Stable High
Concentration Protein Formulations
Csanad M. Varga, Ph.D., Head of Parenteral Formulation Sciences, Millennium Pharmaceuticals
Understanding key degradation pathways is fundamental in the development of high concentration protein formulations. Through targeted experimentation, the dominant mechanisms of instability, whether it be physical or chemical, can be identified and excipient combinations designed and tested. Useful experiments include:
12:00 Close of Morning Session
12:15 Luncheon Workshop (Sponsorship Available) or
Lunch on your Own
 1:45 Chairperson’s Remarks
Tudor Arvinte, Ph.D., School of Pharmacy Geneva-Lausanne, Department of Pharmaceutics and Biopharmaceutics, University of Geneva; Chairman and Chief Executive Officer, Therapeomic, Inc.
 1:50 Practical Formulation Challenges for High-Concentration Proteins
Tapan Das, Ph.D., Senior Principal Scientist, Pfizer Global Biologics
Due to rapid growth in biologics in non-oncology therapeutic areas, there is a growing demand for developing non-intravenous dosage forms such as subcutaneous. Development of a subcutaneous formulation typically requires high protein concentration formulations to accommodate for small volume injections. This presentation will highlight the challenges; discuss technological advancements, and present data from a case study of mAb subcutaneous formulation development.
Understanding the challenges of dose administration in clinical and commercial setting
Requirements to develop a subcu formulation of biologics, especially large proteins
Stability challenges – known and hypothetical concerns, technological bottleneck, DS supply issues
CASE STUDY: MAB HIGH CONCENTRATION
FORMULATION DEVELOPMENT
 2:20 Challenges in Development of High Concentration Antibody Formulation
Hung-Wei Chih, Ph.D., Early Stage Pharmaceutical Development, Genentech Inc.
Treatment of immune system-related diseases using antibodies has been increasing rapidly in recent years. Subcutaneous injection is the preferred route of administration in order to provide convenience to the patients and competitive edge to the product. In order to achieve this goal, development of high concentration formulation is required and also quite challenging. Specifically:
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Challenges in formulation development
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Challenges in manufacturing process
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Challenges in dose administration
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Other concerns
CASE STUDIES
 2:50 How to Effectively Deal with Extractables and Leachables: The Planning and Execution of a Study
Michael Ruberto,
President, Material Needs Consulting, LLC
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What’s currently
being done in the industry in dealing with E&L in formulation
development
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Implementation of some
new technologies for clinical and commercial manufacture using
“disposable container” technology
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Lessons learned in the
planning and execution of a study that looks at extractable/leachables
profiles
3:20 High Throughput Screening of Formulation Buffers to Identify Protein Stabilizing Conditions
Peter A. Leland, Ph.D., Group Leader, Purification & Protein Biochemistry Novagen Brand, EMD Chemicals, Inc.
Production of large quantities of highly pure and active protein is a significant challenge for development of biotherapeutics. Equal to the challenge of production is that of stabilization – defining a formulation that preserves the purity and activity of a biotherapeutic over an extended period of time. Here, we introduce a 96-well protein stability screen based on the differential scanning fluorimetry method. The screen was assembled using elements of fractional factorial and rational design. Using this screen, we have measured the protein stability profile for a wide variety of proteins, including metabolic enzymes, protein kinases, and antibodies. Analysis of results consistently reveals conditions that stabilize a target protein as well as those that destabilize a target protein. Importantly, we have confirmed results from the differential scanning fluorimetry method using differential scanning calorimetry, an analytical method that does not rely on addition of a reporter molecule for measurement of Tm.
3:35 Refreshment Break in the Exhibit Hall
4:30 Importance of Formulation for the Success of Biotech Drugs: Case Studies
Tudor Arvinte, Ph.D., School of Pharmacy Geneva-Lausanne,
Department of Pharmaceutics and Biopharmaceutics, University of Geneva; Chairman and Chief Executive Officer, Therapeomic, Inc.
In spite of large efforts in biotechnology the number of new biotech products reaching the market is not high. Projects may die due to the use of not optimized protein formulations and the failure is falsely attributed to the molecule instead. Examples for the importance of protein formulation for the success of biotech drugs will be presented. The talk will also present newly developed analytical methods to analyze protein aggregation in formulations in conditions as near as possible to those in which the drug is applied in vivo. These “tailor-made” analytical methods are adapted to the necessities of the prinvitrootein formulation rather than to the needs of the analytical techniques.
INTERACTIVE PANEL AND DISCUSSION
5:00 INTERACTIVE PANEL TOPICS:
1. Advantages of outsourcing of formulation for small and large companies
2. Formulation analytic methods
3. Strategies for formulation for early human and POC studies
4. Selection of best projects for development: Interface from research to development
5. Formulation and delivery technologies
Panelists:
Tudor Arvinte, Ph.D., School of Pharmacy Geneva-Lausanne, Department of Pharmaceutics and Biopharmaceutics, University of Geneva; Chairman and Chief executive officer, Therapeomic, Inc.
Kurt Forrer, Ph.D., Senior Fellow, Novartis Pharma AG
Hung-Wei Chih, Ph.D., Early Stage Pharmaceutical Development, Genentech Inc
Kevin King, Ph.D., Director, Formulation Development and Product Enhancements, Global Biologics, Pfizer
Tim Riley, Vice President, PEGylation Research, Nektar
Harald Kropshofer, Ph.D., Global Coordinator & Head Immunosafety, Global Nonclinical Safety, F. Hoffmann La Roche AG
6:00 Reception in the Exhibit Hall
7:00 Close of Day
Overview
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