Bookworm Successful Drug Discovery by János Fischer The IUPAC Subcommittee on Drug Discovery and Development is a section of the Chemistry and Human Health Division (Div VII) of IUPAC. Additional subcommittees are the Subcommittee on Toxicology and that on Clinical Chemistry. I received an invitation to join the drug discovery subcommittee in 1998 from Camille Wermuth, who was a famous professor of medicinal chemistry in Strasbourg. His books are very useful for researchers of medicinal chemistry. “The Practice of Medicinal Chemistry” was published in 1996 by Academic Press, and “The Handbook of Pharmaceutical Salts,” co-edited with Heinrich Stahl, was published in 2002 by Wiley-VCH. The Drug Discovery Subcommittee had several well-known participants from various countries and different companies and academic institutions. Robin Ganellin, professor of medicinal chemistry in London, having founded the Subcommittee, played the most important role both as member and later as leader of this group. He was one of the inventors of cimetidine, the first blockbuster in the history of drug discoveries. It is used for the treatment of heartburn, dyspepsia and hyperacidity. Its commercial use started in 1977 in Europe, and in 1979 in the United States. Robin Ganellin also participated in the discovery of pitolisant, which was approved in Europe in 2016 for the treatment of narcoplesy (it is the subject of Chapter 13 in Volume 3 of ”Successful Drug Discovery” —see below). Robin initiated several projects as the leader of the Drug Discovery subcommittee. I was lucky to have had the opportunity to work with him as co-editor on the book series “Analogue-based Drug Discovery” between 2006-2013.
Leff, Professor Wermuth speaks at a drug discovery meeting in Modena in 2005. At right, Robin Ganellin in 2009, when he presented a lecture in Budapest at the Richter Company.
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Chemistry International
July-September 2020
Three volumes of “Analogue-based Drug Discovery” were published in 2006, 2010, and 2013, and each volume represented a IUPAC project. The first volume included 19 chapters set in three parts. In the first part, Part I, the topic of analogue-based drug discovery was discussed from different viewpoints: Camille Wermuth gave an overview on the analogues and the analogue approach in drug research; John Proudfoot studied the role of drug-like properties in analogue-based drug discovery; and Hugo Kubinyi analyzed the term “privileged structure” and reviewed chemogenomics as a strategy in drug research. Part II consisted of drug class studies and case studies: the main goal was to demonstrate how the activity profile of drugs was optimized within different drug classes. Robin Ganellin described the H2-receptor histamine anatagonists. My task was to write chapters on the HMG-CoA reductase inhibitors, the ACE inhibitors and the angiotensin-II receptor blockers. Several case studies were prepared by key inventors who were The cover designs of the first also members of the IUPAC three editions of Analoguebased Drug Discovery. subcommittee on drug discovery: Gioavanni Gaviraghi described the story of lacidipine, a calcium antagonist. Joerg Senn-Bilfinger wrote a chapter on the discovery of pantoprazole, a proton-pump inhibitor. Rudolf Wiechert summarized the discovery of drospirenone. Part III was a table of analogue classes with the structures and important data of the drugs. (See ref. 1 for a review published in CI) These books were part of an effort to counteract the derogatory use by some commentators of the term “Me-too” drugs. This was part of the approach to
