Thursday, September 29, 2011; 12:30 pm–2:00 pm
Conducted by Deborah Walker, Ph.D., and
Brian Farrer, Ph.D., Merck & Company
Moderated by Caroline McGregor, Ph.D.
Panelist: Annette Bak, Ph.D.
About the Webinar
Enabling formulation technologies can be extremely valuable to test proof of concept for a particular mechanism despite limitations in the pharmaceutical or 'drug-like' properties of tool compounds which have been shown to be potent in vitro.
Formulation development during early drug discovery can involve several challenges particularly limited drug supply, a need for rapid turnaround, and limited development time. It is frequently reported that the percentage of drug candidates that are limited by poor solubility is increasing. These poorly soluble compounds can be challenging and typically require enabling formulations. This trend creates challenges for teams who must drive in-vivo exposures higher for animal toxicology studies. For some mechanisms, there can also be Cmax driven adverse events or a need to maintain plasma exposures for extended periods of time to sustain efficacy which can require formulations to modify the PK profile. Application of versatile formulation tools and drug delivery devices is fast becoming an important tool for the discovery preformulation scientist and many enabling technologies are available for the formulator to consider, including lipids, cosolvents, surfactants, nanoparticles, amorphous solid dispersions, and others.
This webinar reviews various enabling technologies employed to meet the needs of early discovery compounds.
• Alternate material sparing formulation strategies for nanosuspensions
• Small scale amorphous dispersion techniques
• Tablet/capsule formulations for rat studies using SMEDDS and co-solvent matrices
• Medical devices to obtain high exposure for pharmacology studies
• Strategies to modify PK profile such as sustained release formulation and modified dosing regimens
About the Presenters
Deborah Walker is a Research Fellow within the Basic Pharmaceutical Sciences department at MRL Boston. Since starting a small satellite Preformulation group (2005) and as a member of the Basic Pharmaceutical Sciences team (2009), she has made significant contributions to several programs through various stages from discovery to early development and post-PCC support within the Oncology, Neuroscience, Respiratory and Immunology franchises. Deborah has also lead small teams representing functions within Pharmaceutical Sciences and Process Chemistry to enable the transition of clinical candidates through safety studies and FIH. Her current interests focus on the development of analytical tools to enable physical property optimization within early Discovery.
In 1991, Deborah joined Merck Sharpe and Dohme in Australia after completing her B.Sc. at the UTS Sydney. After starting in Quality Operations, she relocated to the US in late 1993 to work in Regulatory and Analytical Sciences in MMD West Point. After obtaining a M.Sc. at Saint Joseph’s University in 1998, she pursued a PhD in chemistry at Princeton University in the laboratory of Professor Daniel Kahne. In 2004, Deborah returned to MMD (Vaccine and Quality Operations) and then joined the Pharmaceutical Research department in MRL as a research chemist in 2005.
Brian Farrer is currently a Research Fellow at Merck in Kenilworth, New Jersey. He has been involved with preclinical formulation since 2003 when he joined Pharmaceutical Chemistry at Merck in Rahway, New Jersey. Current research interests involve controlled release formulation in preclinical space and assessing drug developability. He was an NIH postdoctoral fellow in chemistry at the University of Michigan from 1999 to 2002 where he investigated de novo mettaoprotein design and received his BS from Northwestern University and Ph.D. in inorganic chemistry from the University of North Carolina at Chapel Hill where he studied nucleic acid oxidation. He has authored a number of publications for peer reviewed journals.