Complete Accounts of Integrated Drug Discovery and Development: Recent Examples from the Pharmaceutical Industry Volume 1 Downloaded from pubs.acs.org by 5.8.47.22 on 12/25/18. For personal use only.
Foreword For every drug that is sold on the market, there will be dozens of other drugs that failed somewhere in development, most often as the benefit/risk was simply not good enough to warrant commercialization. Every drug, but also all those which do not crown their development with commercialization, have a story. It starts with a biological hypothesis on the cause for a disease, the development of biological assays, and after the identification of the first hits, the development of these to leads. Then comes the further evolution of the leads to candidates and then finally their progression through the many phases of the development. And when all obstacles are overcome, ultimately we attain commercialization to serve the patient. Every step of the way is complex and involves the interplay of many disciplines, making the discovery and development of a new drug into the biggest and most challenging “science experiment” one can imagine. Each phase of the genesis of a new drug requires the combination of significant scientific insight with the ability to find the creative solutions to the problems and challenges that threaten to derail the process at every step of the way. Many scientific disciplines are involved, but it is the synthetic chemist that is the essential factor. A highly remarkable and insightful description of the uniqueness of chemistry amount the sciences was already suggested in the 19th century by the French scientist Marcellin Berthelot: “La chimie crée son objet. Cette faculté créatrice, semblable à celle de l’art lui-même, la distingue essentiellement des sciences naturelles et historiques.” (“Chemistry creates its object of study. Such a creative power is analogous to the power of art; it essentially distinguishes chemistry from natural and historical sciences.”) Marcelin Berthelot, La synthèse chimique Alcan, Paris, 1887 It clearly describes the central role that we play as chemists. We are the scientists that create. We are not just descriptive and find ourselves with an insurmountable problem, but we have the means to design the solution. This is the same creative process that gives us art, but we chemists are providing a beautifully conceived and prepared organic molecule. The beauty of the creative solution is a molecule with the right properties which ultimately provide the indispensable tool that cures a disease. And the complexity of the creative task, from initially designing the molecule to actually being able to make it safely and economically in large amounts, is covered and described for several examples ix
in this book. The topics encompass drugs that are covering the whole gamut of diseases that inflict mankind: they reach from infectious diseases, systemic disorders, over pain and CNS diseases to various metabolic malfunctions. The long list of diseases clearly demonstrates the strong need for better medicines, created and made by organic chemists. Anybody reading the book will realize the central role that organic chemistry plays in the discovery and development of new drugs. As organic chemists we should be proud of the central role of our science and hope that that the message of Berthelot from 1887 is being recognized again.
Kai Rossen Editor Organic Process Research & Development
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