Innovative approach to drug design that's more likely to result in an approvable drug product Retrometabolic drug design incorporates two distinct drug design approaches to obtain soft drugs and chemical delivery systems, respectively. Combining fundamentals with practical step-by-step examples, Retrometabolic Drug Design and Targeting gives readers the tools they need to take full advantage of retrometabolic approaches in order to develop safe and effective targeted drug therapies. The authors, both pioneers in the fields of soft drugs and retrometabolic drug design, offer valuable ideas, approaches, and solutions to a broad range of challenges in drug design, optimization, stability, side effects, and toxicity. Retrometabolic Drug Design and Targeting begins with an introductory chapter that explores new drugs and medical progress as well as the challenges of today's drug discovery. Next, it discusses: * Basic concepts of the mechanisms of drug action * Drug discovery and development processes * Retrometabolic drug design * Soft drugs * Chemical delivery systems Inside the book, readers will find examples from different pharmacological areas detailing the rationale for each drug design. These examples set forth the relevant pharmacokinetic and pharmacodynamic properties of the new therapeutic agents, comparing these properties to those of other compounds used for the same therapeutic purpose. In addition, the authors review dedicated computer programs that are available to support and streamline retrometabolic drug design efforts. Retrometabolic Drug Design and Targeting is recommended for all drug researchers interested in employing this newly tested and proven approach to developing safe and effective drugs.

The chapters in this volume describe a powerful emerging approach for the therapy of disease. Targeted drug delivery, that is control of the kinetic behavior, tissue distribution, and subcellular localization of pharmaco logically active agents, offers an important means for improving the efficacy of a wide variety of drug therapies. This is particularly true for therapeutic approaches based on newer agents which are the products of recombinant DNA research. These agents, be they peptides, proteins, or oligonucleotides, tend to be larger, more complex, and less stable than traditional drugs. Thus they stand to benefit most from drug delivery systems which can protect them from premature degradation and which can carry them to critical target sites in the body. This volume examines several important aspects of the current state of drug delivery research; it also attempts to project future directions for this field. Successful approaches to drug targeting are based, first of all, on a sophisticated understanding of the biological barriers encountered by the drug-carrier complex as it moves from the portal of administration to the ultimate target site. A second aspect of successful drug delivery is appro priate matching of the disease entity with the pharmacologically active substance and with the delivery system. Thus it is important to be aware of the variety of delivery technologies which currently exist and to be sensitive to their strengths and limitations.