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Acute kidney injury (AKI) is the sudden (over hours or days) loss of kidney function, which may or may not be reversible and may lead to the need for renal replacement therapy with dialysis. AKI represents a potentially life threatening condition with a mortality as high as 80% [1]. Even in those cases that may not be directly life-threatening, the impairment in renal function has significant consequences to the patient. In the setting of AKI, procedures may be limited, drug dosing may be inaccurate, metabolic complications may occur, immune dysregulation is present and all of these may lead to poor outcomes. The therapeutic challenges associated with AKI make prevention critically important as well as prompt, accurate diagnosis and effective treatment when this complication does occur. This issue of Current Drug Targets is devoted to recent developments in the understanding of the pathogenesis of AKI as well as recent advances in the diagnosis and therapy of AKI. The issue begins with an extensive discussion of the epidemiology of AKI by Parmar and colleagues. This review sets the stage for a review of the pathophysiological aspects of AKI in sepsis by Ricci and Ronco. Kalantarinia then discusses the role of imaging and novel imaging techniques in the diagnosis of AKI. Moving into therapeutic regimens, Liu and Glidden provide an overview on why clinical trials for AKI have failed and discuss how the knowledge of past errors in design can be utilized to design an effective clinical trial in AKI patients. The last four articles discuss specific therapeutic agents and their potential in treating AKI. Three of the articles focus on pharmacological agents (the articles by Bajwa et al., Chawla et al., and Gupta et al.), while the final article by Song and Humes, discusses the bioartificial kidney. While no means comprehensive, this issue provides an overview of therapeutic targets for the prevention and therapy of AKI and highlights the movement of these therapies from the bench to the bedside. It is hoped that substantial improvements in the care of patients either at risk for the development of AKI, or in those who have developed AKI will be seen as these advances move into the clinical arena.