CasNo: 138071-82-6
Molecular Formula: C18H31 Gd N4 O9
Description | Gadobutrol is a non-ionic, paramagnetic contrast agent used in magnetic resonance imaging (MRI) to help diagnose issues in the brain, spine, breast, and other parts of the body. It's also used for magnetic resonance angiography (MRA) and to assess blood flow in the heart. Gadobutrol is injected before the MRI and can increase MRI sensitivity for detecting tumors and inflammatory diseases of the central nervous system. |
Uses |
Intravenous gadobutrol [Gadovist™ (EU); Gadavist® (USA)] is a second-generation, extracellular non-ionic macrocyclic gadolinium-based contrast agent (GBCA) that is approved for use in paediatric (including term neonates) and adult patients undergoing diagnostic contrast-enhanced (CE) MRI for visualization of pathological lesions in all body regions or for CE MRA to evaluate perfusion and flow-related abnormalities. Its unique physicochemical profile, including its high thermostability and proton relaxation times, means that gadobutrol is formulated at twice the gadolinium ion concentration of other GBCAs, resulting in a narrower bolus and consequently, improved dynamic image enhancement. Based on > 20 years of experience in the clinical trial and real-world settings (> 50 million doses) and its low risk for developing nephrogenic systemic fibrosis (NSF), gadobutrol represents an effective and safe diagnostic GBCA for use in CE MRI and MRA to visualize pathological lesions and vascular perfusion and flow-related abnormalities in all body regions in a broad spectrum of patients, including term neonates and other paediatric patients, young and elderly adult patients, and those with moderate or severe renal or hepatic impairment or cardiovascular (CV) disease. |
Mechanism of action |
In the central nervous system, Gadobutrol works by highlighting any areas with disrupted blood brain barrier (BBB) and/or abnormal vascularity. In breast tissue, Gadobutrol exposes the presence and extent of malignant breast disease. |
InChI:InChI=1/C18H34N4O9.Ga/c23-12-14(15(25)13-24)22-7-5-20(10-17(28)29)3-1-19(9-16(26)27)2-4-21(6-8-22)11-18(30)31;/h14-15,23-25H,1-13H2,(H,26,27)(H,28,29)(H,30,31);/q;+3/p-3/t14-,15-;/m1./s1
More than two decades of clinical experience has firmly established the diagnostic efficacy and safety of gadolinium-based contrast agents (GBCAs) in contrast-enhanced (CE) MRI to detect pathological lesions throughout the body and in CE MRA to detect peripheral arterial occlusive disease (PAOD) or flow-related abnormalities. As high concentrations of free gadolinium (Gd3+) ions are potentially toxic, all GBCAs are formulated as a central Gd3+ ion surrounded by a linear or macrocyclic chelate ligand.
Median gadobutrol dose was 0.11 mmol/kg body weight. The overall incidence of adverse drug reactions (ADRs) was 0.7 % (n = 170 patients), with similar incidences in patients with renal impairment or cardiac disease, from different geographic regions and in different gadobutrol dose groups. Patients at risk for contrast media reaction had an ADR incidence of 2.5 %. Five patients (0.02 %) experienced serious adverse events, four were drug-related. One patient experienced a fatal anaphylactoid shock, assessed to be related to injection of gadobutrol. The contrast quality of gadobutrol-enhanced images was rated by treating physicians as good or excellent in 97 % cases, with similar ratings in all patient subgroups and indications.
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