Discovery Accelerated
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Chemistry - The Central Science

May 17, 2010 16:36 by EmileBellott

 

  ... AsisChem has developed a seminar  "Medicinal Chemistry and The Roles of Chemistry in Drug Discovery" to show you how to handle the chemistry in your early-stage drug program.


Chemistry is called "The Central Science"  This name was popularized by a late twentieth century chemistry textbook.  People call it the Central Science because understanding of atoms and molecules is built upon the laws of physics and mathematics.  Biology and life processes represent the next rung up the ladder.  The next higher order of conceptual aggregation is built on an understanding of molecules, their properties, and interactions.

In the discovery and development of small-molecule drugs, chemistry is an essential element, every step of the way.  From target validation - to filing an IND - there are tasks that involve chemistry, chemists, chemical synthesis, and chemical testing.

Last month we were invited to UCSF, along with our partner, Apredica, to give a seminar on Drug Discovery --

 



Our piece "Medicinal Chemistry and The Roles of Chemistry in Drug Discovery" used case studies and examples to show how  chemistry is involved from beginning-to-end.  The talk illustrated some of the important opportunities and pitfalls along the way to advancing a new drug candidate.

The final case study described the (published) development of a new non-nucleoside reverse transcriptase inhibitor ( NNRTI ) at Pfizer-UK.

The path wasn't always linear -- they had to take steps forward and back in order to arrive at the final drug candidate, which is now in clinical trials.  Their progress, in terms of IC50, LogP, and half life are shown in the graph.  The Japanese Proverb says: "Fall seven times, get up eight."  Attendees learned how the development team followed this up-and-down prescription, to meet its objectives:

•Improve Half-life
•Improve potency
•Maintain good side effect profile
•Maintain activity against viral mutation
•Create novel IP
•Easily accessible analogs

Due to the overwhelming positive response, we will make our presentation at other universities, and will also present a webinar in June,  for everybody who couldn't attend in person.


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