The human body is continuously exposed to a wide array of structurally diverse chemicals. Such exposure occurs even at the fetal stage as almost all chemicals that are present in the mother’s blood can readily cross the placenta and reach the fetus. Some of these chemicals are ingested voluntarily, for example, medicines and food additives, but the vast majority are taken involuntarily, as environmental contaminants present in the air or in the occupational environment. Undoubtedly, the most important source of such chemicals is the diet, and many dietary constituents have been shown to induce many forms of toxicity including cancer (1 ). Exposure to chemicals is thus inevitable and unavoidable. The body cannot exploit these chemicals either to generate energy or transform them to building blocks and consequently its response is to rid itself of their presence. This chapter discusses the role of drug-metabolizing enzyme systems in this process and the effects of age. The measurement of drug-metabolizing activities is of increasing importance in the safety evaluation of drugs in humans. This chapter describes the use of alkylphenoxazone derivatives for investigating selected activities of drug-metabolizing enzymes.