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April 18, 2012 no comments

Steps to rebuilding pharma R&D efficiency: “The Exupéry Principle” for medicinal chemistry

The efficiency of pharmaceutical R&D is declining.  That much is not in doubt: record R&D expenditure in the last decade has led to fewer drug approvals overall, and almost a complete drought in genuine, first-in-class innovation.  Set aside biologicals, and the performance in small molecules has been even more dire.  But that’s where the unanimity ends.  Dozens of hypotheses circulate to explain the decline in efficiency of small molecule drug development – and every part of the process has come under close scrutiny.

DrugBaron has extensively explored the weaknesses in preclinical and clinical development of the lead compound, but largely ignored the foundation of the whole process: designing the right molecule in the first place.  It turns out that tweaking medicinal chemistry strategies is just as urgent as tweaking development pathways.

“Applying the Exupéry Principle of design to consumer electronics has turned Apple into the world’s most valuable company.  Can it do the same for pharmaceuticals?”

The nub of the problem, it seems, is that pharma companies have overfished the pond.  Talking to visionary medicinal chemist Dr David Fox, I was shocked to discover that less than 1% of stable, easily-made small molecules have ever been synthesised, let alone tested for biological activity.  The other 99% represent virgin territory waiting for those clever enough to seek them out.  If there really are unexplored, unknown continents out there, how do we find them?  DrugBaron asked David Fox, and here is what he had to say…

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