In the central nervous system, Gadobutrol works by highlighting any areas with disrupted blood brain barrier (BBB) and/or abnormal vascularity.

Similarly, gadobutrol is also used in contrast-enhanced magnetic resonance angiography (CE-MRA) for the diagnosis of stroke, detection of tumor perfusion, and presence of focal cerebral ischemia.

[8][10] The most severe reaction to gadobutrol is nephrogenic system fibrosis (NSF) among patients with impaired elimination of the drug.

However, other GBCAs have been shown to cross the placenta in humans and result in fetal exposure, but do not show adverse effects to the fetus.

[8] Animal studies have been conducted in which pregnant rats and rabbits were exposed to 12 and 8 times the human equivalent dose based on body surface area respectively.

The animals were administered multiple doses repeatedly over days, therefore, their exposure levels were much higher than those experienced in humans.

Non-clinical data for Gadrobutrol suggests that less than 0.01% is excreted into breast milk upon intravenous administration of the recommended dose.

For the highest level of safety, breastfeeding should be discontinued for 24 hours upon administration of gadobutrol and any milk properly disposed of.

[8][10] The safety and efficacy data for children under the age of 2 years is limited but has demonstrated that use of the 0.1 mL/kg body weight dose may be used in this population.

These relaxation times, coupled with differences in proton density, are responsible for the variation in intensity of radio frequency signals which contribute to an MRI's tissue visualization capabilities.

[12] The multi-center, randomized, double-blind phase 3 clinical trials (one completed without the active comparator arm)[14] enrolled 402 patients referred for a contrast-enhanced MRI of the CNS, both male and female, over the age of 18.

Pediatric patients, scheduled for a routine contrast-enhanced MRI examination of any body region, both male and female, under the age of 2 years old could be enrolled in the study.

The open-label, multi-center, pharmacokinetic and safety test studied the way gadobutrol was taken into, moved around, and was eliminated from the body of the infants.

Patients referred for a routine magnetic resonance angiography (MRA), both male and female, over the age of 18 years old could be enrolled in the study.

The clinical trial was sponsored by Bayer Healthcare Pharmaceuticals Inc.[17] The only US patent for Gadobutrol is US5980864A, granted in November 1999, to Schering AG.