Iobitridol is a water-soluble, non-ionic, monomeric, low-osmolar, iodine-based contrast medium in which the potential for interaction with membrane proteins in the body has been minimized by stable masking of the molecule's lipophilic tri-iodinated benzene ring. It is approved in various countries worldwide for use as an intravascular contrast medium in adults and children. This article reviews the diagnostic efficacy and tolerability of iobitridol use as an intravascular contrast agent in diagnostic imaging, and briefly overviews its pharmacological properties. In randomized controlled trials, the global image quality and diagnostic quality with iobitridol did not differ from those with other low-osmolar contrast media (iohexol, iopromide, iopamidol, iomeprol and ioxaglate) or the iso-osmolar contrast medium iodixanol in adults or children undergoing radiographic imaging. Large post-marketing surveillance studies have confirmed that iobitridol produces good or excellent opacification and is an effective contrast agent in the vast majority of patients. Iobitridol was generally well tolerated and had a tolerability profile similar to that of other low-osmolar and iso-osmolar contrast media. Thus, iobitridol is an effective intravascular agent for contrast enhancement in diagnostic imaging.