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Drug metabolism and transport are often major sources of inter-individual variability in drug response. Past approaches to managing this biological reality have been to either develop drugs with a wide safety margin or to monitor the patient and adjust doses accordingly. However, decades of research have revealed some of the genetic and environmental causes of variable drug clearance and now promises a new era of individualized drug therapy. Moreover, detailed understanding of reaction mechanisms and structure-activity relationships is opening the door to rational engineering of enzymes for therapeutic and drug development process applications, including the creation of bioreactors for large-scale metabolite synthesis. Recent advances in these and other related research areas form the foundation of this 40th anniversary, 2010 Gordon Conference: “After Forty Years of Inquiry: An Era of Engineered Enzymes and Individualized Drug Therapies”. As in past years, the overall goal of this conference will be to create a collegial atmosphere for both senior and junior scientists in academia and industry to explore the limits of our science, chart new directions that move us beyond existing boundaries, and to create new friendships and collaborations within and across disciplines that will make it a reality. The program will follow the traditional GRC Drug Metabolism format with the keynote lecture Sunday evening, 4 morning sessions with 4 speakers each, 3 evening sessions with 3 speakers each, and Wednesday evening 6 graduate students and postdoctoral fellows will make oral presentations selected from the outstanding posters submitted. Participants are encouraged to submit poster presentations, with the sessions organized by Vice Chair Scott Obach.