The conceptual process of drug discovery is one that is often the result
of an identified need in a defined disease area. This need represents a
mandate from the marketing department of a phar- maceutical company or a
breakthrough at the research level that has agreed applicability in
response to a valid therapeutic demand. Although the intelligent design
and development of new thera- peutic entities, as evidenced by Sir James
Black's H -receptor an- 2 tagonist cimetidine (Tagamet), is
intellectually satisfying, many novel drugs arise from serendipity, from
the chance observation of the research scientist or the clinician, that
a compound has unex- pected actions of use for the treatment of human
disease states. Drugs that have been identified by this route include
the antipsy- chotic chlorpromazine and the putative anxiolytic
buspirone. The events surrounding the process of drug discovery and de-
velopment are the theme of the present volume, which attempts to
present, in a logical and lucid manner, the complexity of a process that
is often naively assumed to represent nothing more than the
identification of a new compound and its rapid introduction into humans,
free of such complications as efficacy, selectivity, safety,
bioavailability, toxicity, and need.