Frontiers
in Medicinal Chemistry
Patrice Talaga, Global Chemistry R&D, UCB
S.A., Belgium
Patrice Talaga -
CV - PDF
In the good old days of drug discovery, medicinal
chemists often performed lead finding and optimization without
having a deep knowledge of the drug target or pathway in mind.
This subjective process, where chemistry driven elaboration
of chemical structures was rather time consuming, actually
delivered many drugs filling the pipelines of many pharma
companies. At that time, in vivo models were extensively used
to directly test the molecules to optimize their biological
responses. Over the recent years, numerous new technologies
e.g. combinatorial chemistry, high throughput screening, high
content screening, in silico visualization tools etc…,
have been setup in order to boost industry’s output.
These technologies, developed during the high throughput era
of “omic” sciences, prompted the medicinal chemists
to synthesize an increased number of so-called “drug
like” compounds. The road taken by the medicinal chemists
has thus become more complex and challenging. Medicinal chemists
today, more than ever, need, in addition to their core expertise
in synthetic organic chemistry, a broad range of expertise
covering computer assisted drug design, cell biology, pharmacology,
formulation science, ADMET, etc…
Unfortunately, this highly interdisciplinary nature of medicinal
chemistry, as well as the numerous new technological advances
aimed to help the medicinal chemists to more rapidly access
drug like compounds, did actually not increase the number
of new drugs which has fallen steadily during the past several
years. This actually happens mainly because of a lack of proven
efficacy and unexpected toxicological side effects that compounds
show in late stage clinical trials. New frontiers in medicinal
chemistry should thus be defined in order to solve the “pipeline
problem” faced by many drug discovery companies. The
land of drug discovery should have its frontiers set-up by
“explorers” of various origins. Thus industrial
medicinal chemists considered as drug maker experts, actually
working according to (too?) strict “drug discovery guidelines”,
should welcome the input of more “naive” and “risky”
explorers from academia, start-ups, and government laboratories,
to redefine the new frontiers in medicinal chemistry.
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