To address the problem of attrition during lead compound discovery and early development, some large drug firms - Pfizer perhaps both the most vocal and committed -- are banking on file enrichment and selection. Better-informed compound library construction and more efficient lead selection could double the useful hit rate, they say, in effect doubling the number of successful new drug introductions downstream. There's room for combining empirical and rational approaches; for example, combining novel fragments to extend diversity with privileged fragments (or scaffolds) that reflect rational assumptions about drug motifs. For now, however, the proposition of file enrichment is much more theory than reality, until it is shown to actually reduce attrition both before and during clinical development, and so improve productivity.
by Mark L. Ratner
Nick Saccomano believes the solution to the pharma industry's R&D productivity problem may well be in hand—enriched chemical files.
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