In the current issue of Drug Metabolism and Disposition (DMD), Dr. Kathleen M. Giacomini, a world-renowned leader in membrane transporter biology, pharmacogenomics, and regulatory sciences, along with and several of her former trainees contribute a special section titled, "New Era of Transporter Science: Unraveling the Functional Role of Orphan Transporters." After obtaining her bachelor's degree in pharmacy from the University of Houston, Dr. Giacomini received her Ph.D. in pharmaceutics from the State University of New York at Buffalo and completed postdoctoral training at Stanford University. She has been a faculty member of University of California, San Francisco (UCSF) since 1982 and was recently named dean of the UCSF School of Pharmacy. She is a cofounder of the International Transporter Consortium, which brings together scientists from academia, industry, and regulatory agencies worldwide to advance knowledge of transporters in drug development with the goal of improving human health. She is also a co-director of the UCSF-Stanford Center of Excellence in Regulatory Science and Innovation in partnership with the US Food and Drug Administration (FDA). Dr. Giacomini is the recipient of numerous awards for her seminal work in membrane transporter genomics and the role these proteins have in drug targeting, disposition, and response. Some of her notable honors include the North American Scientific Achievement Award from the International Society for the Study of Xenobiotics, the Volwiler Research Achievement Award and Paul Dawson Biotechnology Award given by the American Association of Colleges of Pharmacy, the Rawls-Palmer Progress in Medicine Award from the American Society for Clinical Pharmacology and Therapeutics, the Bill Heller Mentor of the Year Award from the American Foundation for Pharmaceutical Education, the Bernard B. Brodie Award from the Division for Drug Metabolism and Disposition of the American Society of Pharmacology and Experimental Therapeutics (Fig. 1), and the Distinguished Pharmaceutical Scientist Award given by the American Association of Pharmaceutical Scientists.Membrane transporters play a major role in human physiology and in drug disposition and response. In 1997, Dr. Giacomini's laboratory cloned and characterized the first human polyspecific organic cation transporter from liver (Zhang et al., 1997), which was almost simultaneously cloned in another laboratory (Gorboulev et al., 1997), and discovered that variants in the gene were associated with the disposition of and response to the antidiabetic drug metformin (Shu et al., 2007). Recently, her group unraveled the functional role of the orphan solute carrier (SLC) 22A24, an anion exchanger that preferentially transports steroid glucuronide conjugates (Yee et al., 2019).Dr. Giacomini trained over 35 graduate students and 30 postdoctoral fellows with many of those trainees becoming national and international leaders in the pharmaceutical sciences. Dr. Sook Wah Yee was a postdoctoral fellow under Dr. Giacomini and is currently a ...