(International Symposium on Laboratory Automation and Robotics) 1998
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Journal of Automated Methods & Management in Chemistry, Vol. 21, No. 3 (May-June 1999) pp. 65-105 Abstracts of papers presented at the ISLAR (International Symposium on Laboratory Automation and Robotics) 1998 The 16th International Symposium on Laboratory Automation and Robotics provided the largest number of technical presentations ever offered at this meeting. State-of-the-art development in laboratory automation and robotics were reflected in the symposium programme which included papers and posters on all aspects of the technology--drug discovery research, data handling and data management, chemical analysis, bio-analytical applications, managing laboratory automation, dissolution testing, pharmaceutical analysis, automation and combinatorial chemistry, validat- ing automated methods and advanced topics. Several new workshops and discussion sessions were included and activated, and provided even more interactive communication. Although the programme was very comprehensive, the Symposium was designed to provide time for both formal and informal exchange of information. The technical presentations were organized into concurrent sessions with grouped papers on related topics. Abstracts for each paper (except two that were not available when going to press) and each poster are included here and the proceedings of the Symposium will be published as a CD-Rom early in 1999. Full presentations of several of these papers will appear in later editions of this journal. Integrating drug discovery technologies The analytical development laboratory provides multiple opportunities for increasing productivity through auto- ames A. Bristol, Parke-Davis Pharmaceutical Research, Ann mation and robotics. Today's generation of analytical Arbor, MI, USA scientists has arrived on the job accustomed to using and The pharmaceutical industry today is entering a new era developing automated approaches to their work. They wherein a number of new and enabling technologies are expect automation, and where it does not exist, will seek maturing simultaneously. These enabling technologies to add it. There are many approaches to automation of include combinatorial chemistry, ultra-high-throughput an analytical technique. The approach can vary depend- screening, genomics, pharamacogenomics, proteomics, ing on the scope and impact of the application, but also data management, high-throughput methodology for whether it is being developed by an analytical scientist or toxicology, and ADME parameters. In addition, new an engineer. A challenge exists in maintaining the and improved automation techniques will have a dra- automation creativity of individual scientists, while pro- matic impact on optimization of these new technologies. viding a mechanism for an integrated and coordinated At the same time, the unprecedented productivity and approach to development within a multi-site, multi- financial success of new pharmaceutical agents and the functional organization. From a diverse mix of analytical effect of mergers leading to vastly larger single companies chemists, biochemists, process control scientists, software have created unprecedented demands for continued developers and mechanical engineers, have come a wide improvements in productivity that will be translated range of automated systems. An overview of these systems directly to increased sales and profits. A further factor will be provided with emphasis on the successes and is the increasing trend to outsource key discovery and challenges of the various development approaches which development activities to biopharmaceutical companies were utilized. The ongoing evolution into the current and contract research organizations. team approach to automation development will be presented. These enabling technologies have the potential to trans- form pharmaceutical discovery into a highly efficient technological advanced process which will demand ap- Quality control: organization, cycle times, compli- propriate resourcing and integration for optimal effi- ance and efficiency ciency. These developments are the challenges for drug discovery scientists in the future who, in addition to j. M. Hawkins, Janssen Pharmaceutica, Titusville, NJ, USA having established expertise within their own scientific Understanding the contributions that the laboratory can disciplines, will necessarily have to work effectively at the make in product/process development, process improve- interface of these intersecting technologies and scientific ment, market surveillance and general business is key to disciplines. the pharmaceutical business today. Poor laboratory practice yields compliance issues, increased cost, in- Coordinated development of multi-site/multi- creased cycle time and delayed product introductions. functional analytical robotics applications: chal- In my presentation, I hope to prompt discussion and gain lenges and visions agreement and recognition of the laboratory's contribu- tion in meeting the expectations of our pharmaceutical E. F. McNiff, Bristol-Myers Squibb, Princeton, NJ, USA customers. I will cover key areas of customer satisfaction, Journal of Automated Methods & Management in Chemistry ISSN 1463-9246 print/ISSN 1464-5068 online (C) 1999 ISLAR 65 http://www.tandf.co.uk/JNLS/auc.htm http://www, taylorandfrancis.com/JNLS/auc.htm Abstracts of papers presented at the 1998 ISLAR the role of the quality control and quality assurance trends towards assay miniaturization, industrial-strength laboratories, measures of accountability and progress, automation and new detection technologies further ex- and an example of how our robotics program is helping tend the view that more is better. However, finding more Janssen meet our goals. leads for more novel targets does not necessarily shorten the time to develop a chemical lead into a drug or increase the likelihood of success for an individual Automation in the lab: does the tail wag the dog? project. Simon Jones, Genetics Institute, Cambridge, MA, USA In the fiture, therefore, an emphasis needs to be placed Intensive automation of repetitive processes in the lab is on using HTS resources and expertise to improve the viewed as an attractive panacea for several reasons. First quality of chemical leads, not simply find more of them. is the assumption that removal of the human element in Concepts in automation, data management and stream- process leads to consistently accurate data sets in a lined assay design which have been developed within the shorter period of time. Second, and deriving from the HTS environment will be applied to other aspects of drug first, is that scientists are 'freed' to focus their talents on discovery, e.g. target validation and secondary screening. more creative pursuits. Third, head count can be stabil- Broader adoption of the tools of HTS may be able to ized and even reduced. Based on this rationale, a virtuous achieve improvements in drug discovery time lines and circle is established that pleases all parties in a biophar- cost savings which cannot occur through more and faster maceutical endeavour. HTS. However, in reality several issues were overlooked and unanticipated problems have arisen. First, and the most Libraries of molecules, screening and optimiza- serious, is the displacement of the bottleneck in sample tion of hits: a cost-effective approach handling to processes up- and downstream of the auto- mated procedure, e.g. data analysis, compound inventory Nigel R. A. Beeley, Amylin Pharmaceuticals, San Diego, CA, and secondary assays in high-throughput screening. USA Second, the daily function of automated units requires As a we need repetitive and accurate operation. This frequently leads product-oriented biotechnology company solutions for libraries of molecules, to the 'burn out' phenomenon and turnover of personnel. inexpensive acquiring data and auto- Third, a substantial financial investment is required not introducing screening robotics, handling only in equipment and bulk materials, but in training mating chemistry when compared to the larger pharma- ceutical and personnel. Fourth, a whole new breed of scientist has companies technology-oriented start-up We now have access to over 250000 com- developed to adapt existing bench processes or create companies. for from the new ones for automated systems. pounds screening purposes following: (i) pharmacophore-based selective purchasing from several These issues and their resolution in small molecule drug purveyors of compounds; (ii) risk-sharing arrangements discovery will be presented. giving access to relatively large numbers of compounds; and (iii) participation in a combinatorial chemistry consortium. We have put in place the necessary infor- The future of in high-throughput screening drug matics and screening robotics to identify hits and analyse discovery data from the above. In addition, we have re-tooled our John Babiak, Robotics and Automation, Wyeth-Ayerst Research, chemistry effort to tbcus on optimization of hits, making Princeton, NJ and Pearl River, NY, USA extensive use of parallel synthesis. Some recent examples from our anti-obesity and anti-diabetic programs will be High-throughput screening (HTS), in conjunction with presented. genomics, combinatorial chemistry and molecular mod- elling, provides pharmaceutical companies with thera- peutic opportunities never before possible. HTS involves The HTS infrastructure---the right tools for the using automated equipment to test a large number of task samples against a novel molecular or cellular target to identify