Clinical Aspects of Biotransformation: An Overview Dedicated to the memory of Mark J. Winn, Ph.D.,1960–1993

Michael Coleman, Louis L. Radulovic

Research output: Chapter in Book/Published conference outputChapter (peer-reviewed)peer-review


The success of a new drug largely depends on the lessons learned from both existing successful and unsuccessful drugs. Although there are many factors that govern the overall effectiveness of a particular agent, its presence for a period commensurate with optimum efficacy is essential at the receptor or tissue and this is governed by clearance. In turn, clearance depends on the myriad processes of biotransformation, which have evolved to serve the individual through biosynthesis and disposal of vital small molecules. Biotransformation is also tasked with protecting homeostasis from xenobiotic agents by removing them, usually through varying degrees of structural alteration aimed at increasing water solubility that promotes renal excretion. This chapter is intended to provide an overview of the major oxidative, conjugative, and hydrolyzing capabilities of our biotransforming enzyme systems, alongside their impressively flexible and highly adapted means of detecting and monitoring small molecules to be metabolized. The role of biotransformation in the insurance of population survival through genetic enzymatic polymorphisms is also explored and its impact on the individual's treatment experience. The effect on biotransformation of inhibition is discussed, as are the major factors the patient brings to the drug treatment process, such as age, disease, gender, and pregnancy. Finally, how the process of drug discovery accommodates biotransformation is outlined from the perspective of the pharmaceutical industry. Understanding of all these interlocking and complex processes will provide an insight into how mass drug therapy can be harnessed to minimize toxicity and maximize efficacy in the twenty‐first century.
Original languageEnglish
Title of host publicationEncyclopedia of Drug Metabolism and Interactions,
Subtitle of host publication Volume 6, Clinical Aspects
EditorsMichael Coleman, Louis Lazo Radulovic
ISBN (Print)978-1-118-14979-9
Publication statusPublished - 2012


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