A Comprehensive Monograph on Gadobutrol (Gadavist®/Gadovist®): Chemical Properties, Pharmacology, Clinical Efficacy, and Safety Profile

Executive Summary

Gadobutrol is a second-generation, gadolinium-based contrast agent (GBCA) that holds a prominent position in the field of diagnostic magnetic resonance imaging (MRI). Structurally, it is classified as a non-ionic, macrocyclic chelate, a design that confers exceptional stability and is central to its distinguished safety profile. The gadolinium ion (Gd3+), the paramagnetic component responsible for contrast enhancement, is securely encapsulated within a rigid macrocyclic ligand framework, dihydroxy-hydroxymethylpropyl-tetraazacyclododecane-triacetic acid (butrol). This structure significantly minimizes the in vivo release of toxic free gadolinium, placing Gadobutrol in the lowest-risk category for the rare but severe condition known as nephrogenic systemic fibrosis (NSF).

A key distinguishing feature of Gadobutrol is its unique formulation at a concentration of 1.0 mmol/mL, which is double that of most other GBCAs. This high concentration, combined with its intrinsically high T1 relaxivity, allows for the administration of a smaller injection volume to achieve robust contrast enhancement. This property is particularly advantageous in advanced imaging applications such as dynamic contrast-enhanced MRA and perfusion MRI, where a tight, concentrated bolus of the contrast agent is critical for optimal diagnostic image quality.