So it’s true that they’re not everyone’s Christmas present, but I wanted to do my yearly roundup of books on medicinal chemistry and drug discovery. This list builds on last year’s recommendations, with updated editions of some titles, and adds a number of suggestions from readers.
A relatively recent (2011) history of our whole field is <The Evolution of Drug Discovery. There are many books written at various levels about the discovery of particular drugs or therapies, but it’s rare to see the entire business of drug discovery covered like this.
For general medicinal chemistry, you have Bob Rydzewski’s Real World Drug Discovery: A Chemist’s Guide to Biotech and Pharmaceutical Research from 2008. And from 2013, there’s Drug Discovery: Practices, Processes, and Perspectives, by Jack Li and E. J. Corey. Another recommendation from several readers is Textbook of Drug Design and Discovery by Krogsgaard-Larsen et al. Several readers here have also recommended earlier versions of Silverman’s medicinal chemistry book, and now in its third edition: The Organic Chemistry of Drug Design and Drug Action. Readers have also recommended Camille Wermuth’s The Practice of Medicinal Chemistry, and it’s now in its fourth edition for 2015. Update: another one, just published in November, is Small Molecule Medicinal Chemistry: Strategies and Technologies. For getting up to speed, several readers recommend Graham Patrick’s An Introduction to Medicinal Chemistry (2013). Similarly, Medicinal Chemistry: The Modern Drug Discovery Process (Pearson Advanced Chemistry) is a recent introductory textbook that I found to be well written.
Process chemistry is its own world with its own issues. Recommended texts here are Practical Process Research and Development – A guide for Organic Chemists by Neal Anderson (2012). Repic’s Principles of Process Research and Chemical Development in the Pharmaceutical Industry is older (1998), but comes recommended as well. Another recommended text is Process Development: Fine Chemicals from Grams to Kilograms (Oxford Chemistry Primers) by Stan Lee (no, not that Stan Lee) and Graham Robinson. On an even larger scale, McConville’s The Pilot Plant Real Book is subtitled “A Unique Handbook”, and it comes recommended by readers here, too.
Case histories of successful past projects can be found in Drugs: From Discovery to Approval by Rick Ng, now in a new 2015 edition, and also in Walter Sneader’s Drug Discovery: A History. A recent addition to this area is Hallelujah Moments: Tales of Drug Discovery by longtime medicinal chemist Gene Cordes.
Another book that focuses on a particular (important) area of drug discovery is Robert Copeland’s Evaluation of Enzyme Inhibitors in Drug Discovery: A Guide for Medicinal Chemists and Pharmacologists, and readers have specifically mentioned it as useful. Other recent books on particular areas of med-chem are Bioisosteres in Medicinal Chemistry, Volume 54 by Brown et al., recommended by several readers, Scaffold Hopping in Medicinal Chemistry, Prodrugs and Targeted Delivery: Towards Better ADME Properties, and Protein-Protein Interactions in Drug Discovery.
For chemists who want to brush up on their biology, readers recommended an earlier edition of this Terrence Kenakin book: A Pharmacology Primer: Techniques for More Effective and Strategic Drug Discovery, as well as his Pharmacology in Drug Discovery: Understanding Drug Response. Joseph Cannon’s Pharmacology for Chemistshas also been recommended.
Overall, one of the most highly recommended books across the board comes from the PK end of things: Drug-Like Properties: Concepts, Structure Design and Methods from ADME to Toxicity Optimization by Kerns and Di, which is the new edition coming out in early 2016. The same authors recently published Blood-Brain Barrier in Drug Discovery: Optimizing Brain Exposure of CNS Drugs and Minimizing Brain Side Effects for Peripheral Drugs as well. Another recent PK-centric book is Lead Optimization for Medicinal Chemists: Pharmacokinetic Properties of Functional Groups and Organic Compounds. For getting up to speed in this area, there’s Pocket Guide: Pharmacokinetics Made Easy (Pocket Guides) by Donald Birkett, which will not make all your pharmacokinetics problems easier, but will at least give you the tools to understand what’s going on, and the Drug Metabolism and Pharmacokinetics Quick Guide, which has also been recommended.
In a related field, standard textbooks for toxicology are Casarett & Doull’s Toxicology: The Basic Science of Poisons and Hayes’ Principles and Methods of Toxicology. A book on its application to drug development is Preclinical Safety Evaluation of Biopharmaceuticals: A Science-Based Approach to Facilitating Clinical Trials, from 2008.
Jerrold Zar’s Biostatistical Analysis comes recommended, and it’s a field that a lot of people (including me) could stand to be better at. For getting into this area, try Essential Biostatistics: A Nonmathematical Approach.
A book I reviewed last year might prove useful as well: Navigating the Path to Industry: A Hiring Manager’s Advice for Academics Looking for a Job in Industry, aimed at academic scientists (not just entry-level ones, either) who are looking at industrial research positions and wondering how to get from here to there. Similarly, I very much enjoyed A Practical Guide to Drug Development in Academia, finding it full of very worthwhile advice for academic researchers looking to get into the pharma world with their own research.