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Day Two
Friday, January 16
7:30am – 4:00pm Registration Open
7:30 Breakfast Workshop (Sponsorship Available)
8:15 Chairperson’s Remarks
Christopher A. Rhodes, Ph.D., Executive Director, Pharmaceutical Sciences, Amylin Pharmaceuticals
NOVEL DRUG DELIVERY APPROACHES
 8:20 Improving Biotherapeutic Convenience and
Compliance through Delivery Technologies
Christopher A. Rhodes, Ph.D., Executive Director, Pharmaceutical Sciences, Amylin Pharmaceuticals
The full potential of parenteral products can only be realized through a clear understanding of the patient and physician interface with the product. Strategies for improving the presentation of biotherapeutic products will be discussed including technologies designed to reduce injection frequency and allow non-injectable administration. Technologies to reduce Injection frequency can be divided in two categories: sustained release formulations and sustained circulation molecular modifications. Technologies for non-injectables can be broken down into transdermal systems and oral, nasal, and pulmonary systems. The challenges and opportunities in applying these technologies will be discussed.
 8:50 PEGylation Strategies for Improved Protein Formulations
Tim Riley, Vice President, PEGylation Research, Nektar
 9:20 Elastin-like Biopolymers: A Uniquely Versatile
Scaffold for Optimizing Drug Delivery
Ariel Boutaud, Ph.D., Director, Research, PhaseBIO
Elastin-like repeat sequences (ELPs) can be engineered to undergo a controlled phase transition from a soluble to an insoluble state, a process that is fully reversible. Depending on how the biopolymers are designed, soluble fusion constructs are produced for prolonging half-life and targeted delivery or insoluble constructs (post injection) for depot formulation and sustained release. This allows selection of whichever delivery mechanism provides the best pharmacological profile for a chosen drug target. The technology is broadly applicable to peptides, proteins and small molecule drugs.
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Major hurdles in the industry are to lower costs of goods, improve efficacy, safety and convenience of administration. This technology addresses all of these challenges.
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Attendees will gain an understanding of the technology to make next generation pharmaceuticals with the attributes above.
9:50 Coffee Break in the Exhibit Hall
10:45 Poster Awards in Exhibit Hall
 11:00 DepoFoam Multivesicular Liposomal for the
Delivery of Proteins and Peptides
Bill Lambert, Ph.D., Senior Vice President, Pharmaceutical Development, Pacira Pharmaceuticals, Inc.
DepoFoam is an aqueous suspension of multivesicular liposomes (MVL) which can be utilized for many routes of administration including subcutaneous, intraarticular, intraperitoneal, intrathecal, epidural, subconjuctival, and intraocular. While DepoFoam formulations have been successfully applied commercially for traditional pharmaceuticals, one of the more promising applications of DepoFoam is for the sustained systemic delivery of proteins, which generally have short plasma half-lives. Examples of sustained release formulations of proteins will be provided, including myelopoietin (a 35kD IL-2/G-CCSF chimeric protein) and interferon alpha-2b (IFNα-2B). Once a week subcutaneous formulations with little or no initial burst have been demonstrated in rats for both of these proteins.
The audience will understand the advantages of this system relative to other sustained release systems such as:
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How the unique honeycomb structure of DepoFoam can be utilized for a broad variety of drugs
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The ability to be used with narrow gauge needles and pen systems
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Excellent toleration and minimal burst
 11:30 Stabilization, Manufacture and Packaging, and Delivery of Proteins, Antibodies, Vaccines, and Biologics
Robert Sievers, Ph. D., Professor, of Chemistry and Biochemistry,
University of Colorado at Boulder
We have invented and are testing new methods of stabilizing and drying microparticles that are faster and less expensive alternatives to lyophilization. As a case study, we are concluding pre-clinical testing of a needle-free inhalable measles vaccine in rodents and non-human primates, in which unidose blisters have been successfully used to preserve, then deliver into masks, aerosols of live attenuated measles virus vaccines, as part of the Grand Challenges in Global Health Inititiative. Plaque neutralization studies have demonstrated the generation of robust mucosal immune responses in the respiratory tracts. The vaccine can be made and delivered for less than 26 cents per delivered dose and needs no water-for-injection for reconstitution, which occurs in the moist respiratory tract. No batteries or electricity are needed.
PROCESS AND PRODUCTION CHALLENGES
12:00 Overcome Current Challenges in mAb Drug Product Production
Tim Tressel, Ph.D.,
Director, Purification Process Development, Amgen, Inc.
Recombinant monoclonal antibodies (mAbs) are important therapeutics in treating variety of diseases. Innovation has been the engine leading to continual discovery and improvements in mAb production process. In this presentation, common mAb therapeutics production steps including upstream and downstream process are reviewed and major challenges in mAb formulation during the process are discussed. Discoveries and methods of addressing the stability of monoclonal antibodies to TRP light oxidation, and uneven distribution of polysobate-20 absorbed by aseptic filters during processes of drug substance and drug product are presented. Potential factors leading to mAb particle formation are proposed.
12:30 Close of Morning Session
12:45 Luncheon Workshop (Sponsorship Available) or
Lunch on your Own
2:00 Chairperson’s Remarks
ENABLING ANALYTICAL METHODOLOGIES
 2:05 Potential Impact of Formulations on the Immunogenicity of Biologics
Harald Kropshofer, Ph.D., Global Coordinator & Head Immunosafety, Global Nonclinical Safety, F. Hoffmann La Roche AG
Many different factors have been reported that could potentially impact the incidence of anti-drug antibody related immunogenicity: the drug substance itself, the formulation, the route of administration, the drug target, the genotype of the patient, the indication and other aspects which are less well understood. It is still open which types of aggregates do elicit immune responses and which immunological mechanisms apply. The presentation will put emphasis on The immunological rationale for protein aggregates becoming visible for the immune system
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The high complexity of protein aggregation
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The uniqueness of each drug substance with respect to its interactions with the immune system
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New in vitro tools to address drug-induced modulation of human immune cells
 2:35 Characterization of Degradation Pathways
Anne Kowal, Ph.D., Associate Director, Analytical Development,
Millennium
The degradation pathways of biologics can be extremely complex, so a variety of different analytical methods are required to examine the overall stability of a molecule. The ability to select the most appropriate methods for monitoring potential changes in a molecule at early stages of development may poses one type of challenge. At later stages of product development, building the tools to characterize the degradation pathways offers another. Some examples of the approaches used to examine biologics stability and degradation profiles will be presented.
 3:05 Novel Methods and New Technologies for Detecting and Characterizing Aggregates in
Protein Therapeutics
Tapan Das, Ph.D., Senior Principal Scientist, Pfizer Global Biologics
Protein aggregation is one of the major concerns in biologics development for quality issues and safety concerns due to potential immunogenicity. Protein aggregation occurs in a wide range of size and forms, thereby posing a huge analytical challenge of detection and characterization. This presentation will highlight some of the recent advances and discuss with few examples how understanding of aggregation pathway can be improved.
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Discussion of the aggregation related concerns
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Understand present status of aggregation research in biotherapeutics
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Emerging techniques
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Some examples of aggregate and particulate characterization
 3:35 A Case Study Detailing the Application of Analytical Methods to Characterize Protein Aggregation for a Biopharmaceutical Drug Program
Steven C. Pomerantz, Ph.D., Senior Research Scientist, Discovery Mass
Spectrometry, Centocor R&D
Jennifer F. Nemeth-Seay, Ph.D., Principal Research Scientist, Head, Discovery Mass Spectrometry, Centocor Research and Development
The expression and purification of protein drug candidates is a complex process that does not produce just the expected product, but by-products as well. Often, drug impurities such as protein clips, multimers, or aggregate, are also produced. In order to fully understand the composition of a protein product, which could be a combination of all the above species; as well as to improve future production methods; it is important to characterize these other protein forms during the course of development. In this case study, a variety of analytical techniques including SDS-PAGE gels, size-exclusion chromatography (SEC), SEC-static light scattering (SLS), free-thiol analyses, and mass spectrometry were used to characterize aggregate found in multiple lots of material of a biopharmaceutical drug candidate. The information is being used to improve product yield and the purification process.
4:05 Closing Comments and Conference Wrap-up
4:30 pm Close of PepTalk
Overview
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