ABSTRACT

Iodinated contrast agents used for radiographic procedures are

unique pharmaceuticals. They are available as highly concentrated

solutions that are administered at high doses; this is possible

because of their high safety profile and special physicochemical

properties (high hydrophilicity and inertness). The currently used

iodinated contrast agents can be divided into two classes based on

their chemical structure.Monomeric agents are composed of a single

triiodinated benzene ring, whereas dimeric agents consist of two

covalently linked triiodinated benzene rings [1]. The passage from

ionic to neutral systems has markedly improved their safety profile,

making adverse reaction to their administration rare events [2].

Besides their capability to induce contrast in computed tomography

(CT) images, owing to the presence of high X-ray adsorbance iodine

atoms, the concomitant presence of amide groups has driven an

interest in their exploitation as magnetic resonance imaging (MRI)-

chemical exchange saturation transfer (CEST) agents. In seeking

routes to accelerate the entry of CEST agents into clinical practice,

it has been rather straightforward to consider chemicals already

approved for human use and potentially able to generate CEST

contrast. On this basis, a systematic study of currently used X-

ray contrast agents containing mobile protons (e.g., Iopamidol-

Isovue R© Bracco Imaging SpA, Italy; Iopromide-Ultravist R© BayerSchering AG, Germany; and Iobitridol-Xenetix R© Guerbert, France) has been undertaken. The in vivo results obtained so far appear very

encouraging for clinical translation of these CEST agents.