This is the first-ever guide to protease inhibitor drug design, tying together the knowledge gained from numerous recently developed protease drugs in a single source. The first part provides a general introduction to the protease family, including its physiological functions and molecular structure. A discussion of the molecular mechanism leads on to the rational design of inhibitors, which is covered in the second part. The third and largest section presents various case studies of successful protease inhibitor drug development programs, as well as current uses of such inhibitors in pharmaceutical medicine. A ready reference aimed primarily at professionals in the pharmaceutical industry, as well as for anyone studying proteases and their function.