Dynamic contrast-enhanced magnetic resonance imaging (DCE-MRI) is performed after the administration of intravenous contrast medium to noninvasively access tumor vascular characteristics. DCE-MRI techniques utilizing low-molecular-weight contrast media have successfully made the transition from methodological development to preclinical and clinical validation and are now rapidly becoming mainstream clinical tools. DCE-MRI using macromolecular contrast medium (MMCM) can also assay microvascular characteristics of human tumor xenografts. MMCM approval for human use will occur soon. The success of both techniques depends on their ability to demonstrate quantitative differences of contrast medium behavior in a variety of tissues. Evidence is mounting that kinetic parameters correlate with immunohistochemical surrogates of tumor angiogenesis, including microvessel density, and with pathologic tumor grade. DCE-MRI is being applied to monitor the clinical effectiveness of a variety of treatments, including antiangiogenic drugs. Kinetic parameter changes following treatment have correlated with histopathological outcome and patient survival. This article reviews the current clinical status of low-molecular-weight DCE-MRI and reviews the potential of MMCM techniques for evaluating human tumors. Ongoing challenges faced by DCE-MRI as clinical and research tools will be explored. J. Magn. Reson. Imaging 2002;16:407–422. © 2002 Wiley-Liss, Inc.