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Editor's note: Mike Williams is adjunct professor at Northwestern University in Chicago, from where he publishes his personal views on today's drug discovery industry.
For the better part of the past three decades, interest in natural products as potential sources for new drugs has been overshadowed by an overtly mechanistic, targephilic approach to identifying new chemical entities (NCEs) as potential leads for new drugs.
The Targephilic Approach
This approach involves the screening, via high-throughput screening (HTS), of libraries of small molecules in massive numbers against selected targets expressed in vitro. This is done in anticipation of identifying NCEs active at a discrete molecular target that could be optimized for potency, efficacy, selectivity and drug-like properties.
Since these NCEs would ostensibly be selective in their target interactions, it was an a priori assumption that their side effect liabilities would be reduced if not eliminated. Drug discovery would thus become faster and more cost effective. This approach was supported by robotics-based HTS assay systems and by newer chemistry technologies, covered under the rubric of "combichem," which involved the facile synthesis on an industrial scale of thousands to millions of compounds. A focus on making compounds that could be made rather than those that should be made markedly limited the useful contributions from combichem such that it now has been replaced by the infinitely more productive parallel library synthesis approach, with a greater emphasis on NCEs that have drug-like properties.
To many in the pharmaceutical industry, the reductionistic nature of the targephilic approach played a major role in the dearth of new drug approvals. This is reflected in the comment attributed to Martin MacKay, Pfizer Inc.'s head of research, after the January 2009 layoff of 800 researchers that "nobody in the industry is happy with our productivity."
It also can be seen in New York-based Pfizer's subsequent acquisition of Wyeth for a record $68 billion, with five-figure layoffs in the offing. Pharma now is in the throes of necessarily rediscovering a more holistic, pharmacology-based approach to drug discovery. Not so the federal government.
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For the better part of the past three decades, interest in natural products as potential sources for new drugs has been overshadowed by an overtly mechanistic, targephilic approach to identifying new chemical entities (NCEs) as potential leads for new drugs.
The Targephilic Approach
This approach involves the screening, via high-throughput screening (HTS), of libraries of small molecules in massive numbers against selected targets expressed in vitro. This is done in anticipation of identifying NCEs active at a discrete molecular target that could be optimized for potency, efficacy, selectivity and drug-like properties.
Since these NCEs would ostensibly be selective in their target interactions, it was an a priori assumption that their side effect liabilities would be reduced if not eliminated. Drug discovery would thus become faster and more cost effective. This approach was supported by robotics-based HTS assay systems and by newer chemistry technologies, covered under the rubric of "combichem," which involved the facile synthesis on an industrial scale of thousands to millions of compounds. A focus on making compounds that could be made rather than those that should be made markedly limited the useful contributions from combichem such that it now has been replaced by the infinitely more productive parallel library synthesis approach, with a greater emphasis on NCEs that have drug-like properties.
To many in the pharmaceutical industry, the reductionistic nature of the targephilic approach played a major role in the dearth of new drug approvals. This is reflected in the comment attributed to Martin MacKay, Pfizer Inc.'s head of research, after the January 2009 layoff of 800 researchers that "nobody in the industry is happy with our productivity."
It also can be seen in New York-based Pfizer's subsequent acquisition of Wyeth for a record $68 billion, with five-figure layoffs in the offing. Pharma now is in the throes of necessarily rediscovering a more holistic, pharmacology-based approach to drug discovery. Not so the federal government.
Read the full story here
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