The Impact of Technological Advances on Drug Discovery Today
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0092-86 I5/2001 Copyright 0 2001 Drug Information Association Inc.
THE IMPACT OF TECHNOLOGICAL ADVANCES ON DRUG DISCOVERY TODAY ESTHERF. SCHMID,PHD Strategic Planner Discovery
KEITH JAMES,PHD Vice President Discovery
DENNISA. SMITH,PHD Senior Director, Drug Metabolism Sandwich Laboratories, F‘fizer Global Research and Development, Sandwich, Kent, United Kingdom
In recent years, technological advances have changed the face of drug discovery beyond recognition. New compounds can now be synthesized in unprecedented numbers via combinatorial chemistry, matched by ultra-high throughput screening of unparalleled speed and scope. Until recently, this has been divorced and almost in opposition to the traditional structure activity relationship (SAR) lead synthesis programs (open termed rational design). A further evolution is now occurring, combining the synthetic and screening revolution, but with the high speed synthesis directed by emerging SAR in a “closed loop, ” thus allowing rapid optimization of chemical mattel: Despite these impressive advances, the debate is still ongoing as to whether the industrialization of drug discovery will increase the output of launched New Chemical Entities with higher and higher hurdlesfor drug safety measures of eflcacy and outcomes. In addition, the sequencing of the human genome has started its own, very costly, highly competitive and resourceconsuming race to assign function to novel genes. The industry will need to change the way discovery and development work together to succeed in an increasingly uncertain environment. Key Words: Industrialization; High throughput screening; Drug discovery; Combinatorial chemistry; Drug development
INTRODUCTION
small molecule endogenous agonists, in particular biogenic amines, provided useful insights into potential disease processes. This could be exploited by pharmacologists by triggering functional responses in tissue preparations through natural or synthetic agon& In addition, many of these endogenous agonists were highly amenable to rational conversion into h p - l i k e antagonists via medicinal chemistry. Despite the low technology, low throughput, and low target numbers in this scenario, for the pharmaceutical industry, as well as for patients, it has
CoNVENT1oNAL DRUG DISCoVERY used to be a process’ Even though the molecu1ar target was not always known, a growing understanding of
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Presented at the DIA 36th Annual Meeting, June 1115, 2000, San Diego, California. Reprint address: Dr. Esther Schmid, Discovery HQ, IPC 924, Sandwich Laboratories, PGRD, Ramsgate Road, Sandwich, Kent ~ ~ 9NJ, 1 3UK, E--L Esther-Schmid@Sandwich. Wizer.com.
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Esther F. Schmid, Keith James, and Dennis A. Smith
proven to be a major success story. Approximately 500 New Chemical Entities (NCEs) were approved in the United Kingdom since 1972, which have originated from such conventional drug discovery (1). In fact, between 1961 and 1987, approximately 1900 NCEs which target approximately 500 distinct proteins were brought to market worldwide (2).
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