09:00 Chairperson’s Welcome and Opening Address

Analysis of the Current Opportunities within the Development of Polymorphic Screening Methods as we Search for New, Stable Polymorphs and the Hurdles Faced Along the Way

09:10 Case Study: Finding Crystal Forms That Matter

• Optimising drug product performing through solid form screening and selection
• Case studies in finding commercially viable crystalline forms

Susan Reutzel
Senior Research Advisor
Eli Lilly and Company

09.50 Case Study: Discovery and Selection of an Optimal Crystal Form for the Various Stages of Pharmaceutical Development

Selection of an optimal crystalline form of an active pharmaceutical ingredient plays a critical role in the different stages of drug development impacting bioavailability, solubility, stability, and other physical properties of a drug candidate. Identification and evaluation of solid phases of a drug are critical in defining a stable platform for robust processing from bench scale to plant scale manufacturing and formulation.

• A proactive, collaborative approach between development groups can have a tremendous impact on the likelihood of a candidate to achieve maximum return on investment. Topics of discussion include:
• Planning the optimum time to begin crystal form screening activities. Focus on the depth of experimental activities based on the development stage of the compound.
• Selection of a crystal form with acceptable properties for the stage of development targeted.
• Case studies involving analysis of useful phases of a drug substance and impacts of form selection to define practical and efficient processes.

Michael McNevin
Molecular and Materials Characterisation
Merck

11:00 Case Study: Polymorphism and Impurities : A Delicate Interplay of Physical and Analytical Chemistry

• Case study of an atypical polymorph screen
• How the presence of impurities can trouble a polymorphic investigation
• The need of a critical view on the analytical methods used

Luc Aerts
Associate Director of Solid State Characterisation and Development
UCB Pharma

11:40 Interactive Round Table Discussions

A: Continuous Crystallisation

James Evans
Associate Director
Novartis-MIT Centre for Continuous Manufacturing

B: Speeding Up Scale Up From Lab to Pilot

Zoltan Nagy
Professor of Process Systems Engineering
University of Loughborough

C: Control of The Crystallisation Process

Mei Lee
Investigator
GlaxoSmithKline

D: Assessing Stability of Polymorphs

Peter Wood
Research and Application Scientist
Cambridge Crystallographic Data Centre

13:20 Solid Form Informatics: Knowledge-Based Tools to Assess Risk & Inspire Development

Quality by Design is becoming increasingly important in the Pharmaceutical Industry with more focus being placed on control and understanding of polymorphism. Solid Form Informatics makes use of the vast amount of solid state interaction data in the Cambridge Structure Database to provide predictive analytics in the area of substance development and risk assessment. This presentation aims to show how these methods can provide the following:

• Improved planning due to early indication of potential polymorphism issues
• Decision support regarding the need for further polymorph screening
• Independent assessment of polymorph results from collaborations or contract services
• Improved efficiency and effectiveness of identifying suitable salts and co- formers

Peter Wood
Research and Application Scientist
Cambridge Crystallographic Data Centre

14:00 European Patient Office: Patenting Polymorphs at the European Patent Office

• How to assess if a new polymorph is patentable
• What format for polymorph patent claims will the EPO consider
• Overcoming typical approval objections to patent applications and taking steps to avoid complications
• Recent case law from the EPO's Board of Appeal

Emmeline Marttin
Patent Examiner
European Patent Office

15:10 Managing Physical Forms: Analytical and regulatory considerations

• Discussion of guidelines dealing with polymorphism (ICH, Pharmacopoeia monographs) and there impact on the pharmaceutical development of solid forms
• Control of polymorphic forms and need qualitative and quantitative analytical methods
• What are some physical-chemical properties of polymorphs that are of concern?
• Must you be able to quantitative polymorphs in drug substance and drug products?

Michael Mutz
Senior Fellow
Novartis

15:50 A Fully Automated Crystallisation Screening System at AstraZeneca

• A presentation of a fully automated system, which can handle all sorts of small scale crystallization experiments, including salt, polymorph, and co-crystal screening
• An overview of the design principles and experimental capabilities of the equipment
• A discussion of the applied methodology for medium throughput salt and polymorph screening

Martin Bohlin
Principal Scientist, Crystallisation
AstraZeneca

16:40 Chairperson’s Closing Remarks and End of Conference