gadofosveset

Action and Spectrum

Actions and Spectrum: 

gadofosveset is a contrast agent in magnetic resonance imaging (MRI) procedures. It is a gadolinium-based contrast agent (GBCA) designed explicitly for imaging blood vessels.  

Action:  

• gadofosveset works by altering the magnetic properties of blood, which enhances the visibility and differentiation of blood vessels during MRI scans. It is administered intravenously and rapidly binds to albumin, a protein found in the blood. This binding extends the half-life of gadofosveset in the bloodstream, allowing for a longer imaging window compared to other GBCAs. 

Spectrum:  

• gadofosveset has a broad spectrum of applications in vascular imaging. It is primarily used for evaluating vascular structures and detecting abnormalities in the cardiovascular system. It provides detailed visualization of blood vessels, including arteries, veins, and capillaries. gadofosveset-enhanced MRI scans can help diagnose conditions such as arterial stenosis (narrowing), aneurysms, arteriovenous malformations, and tumors involving blood vessels. 

Drug Interaction

Adverse Reaction

Frequency defined 

1-10% 

Headache 

Pruritus  

sensation of cold  

Nausea  

burning sensation 

Bruising at the injection site 

Dizziness 

dysgeusia  

paresthesia 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

• Known hypersensitivity: gadofosveset should not be administered to individuals with a known history of hypersensitivity or allergic reactions to gadolinium-based contrast agents (GBCAs).  
• Severe renal impairment: gadofosveset is predominantly eliminated through the kidneys, and individuals with severe renal impairment (glomerular filtration rate, or GFR, less than 30 mL/min/1.73 m²) may be at an increased risk of nephrogenic systemic fibrosis (NSF). NSF is a rare but severe condition characterized by fibrosis of skin, muscles, and internal organs. Therefore, gadofosveset should be avoided in patients with severe renal impairment. 
• Acute kidney injury: gadofosveset should not be used in patients with acute kidney injury or any other condition that may result in an acute deterioration of renal function. This is because impaired renal function can affect the clearance of the contrast agent from the body, potentially leading to higher gadolinium concentrations and an increased risk of adverse events. 
• Pregnancy and breastfeeding: Using gadofosveset during pregnancy is generally not recommended unless the potential benefits outweigh the risks. Similarly, it is advised to avoid breastfeeding for 24 hours following gadofosveset administration to prevent the transfer of the contrast agent to the infant through breast milk. 

Caution 

• Renal impairment: Individuals with mild to moderate renal impairment (GFR 30-89 mL/min/1.73 m²) should exercise caution when receiving gadofosveset. Although the risk of developing NSF is lower than other GBCAs, there is still a potential risk. Close monitoring of renal function is necessary for these patients. 
• Allergic reactions: While rare, allergic reactions can occur following the administration of gadofosveset. Patients should be monitored for any signs of allergic response during or after the injection, including rash, difficulty breathing, itching, or swelling of the face, lips, tongue, or throat. Immediate medical attention should be sought if any allergic symptoms occur. 
• Extravasation: Care must be taken to avoid the extravasation, which is the leakage of gadofosveset into the surrounding tissues during injection. Extravasation can lead to local tissue irritation or injury. Healthcare professionals should closely monitor the injection site and take appropriate measures to decrease the risk of extravasation. 
• Interactions with other medications: gadofosveset may interact with certain medications, particularly those that affect renal function or other agents that can be nephrotoxic.  
• Pediatric and geriatric populations: The safety and efficacy of gadofosveset in pediatric and geriatric populations have not been extensively studied. Caution should be exercised when using gadofosveset in these age groups, and the potential risks and benefits should be carefully evaluated. 

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: C 

Lactation:   

Excreted into human milk: Not known. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    
• Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

gadofosveset is a gadolinium-based contrast agent (GBCA) used in magnetic resonance imaging (MRI) procedures. It is administered intravenously and rapidly binds to albumin, a protein found in blood, extending its half-life in the bloodstream. gadofosveset alters blood’s magnetic properties, enhancing blood vessels’ visibility during MRI scans. It has a high relaxivity, allowing for enhanced contrast in MRI images.

The contrast agent circulates in the bloodstream and gradually diffuses into the extravascular interstitial space, providing visualization of vascular permeability and tissue enhancement. gadofosveset is predominantly eliminated through the kidneys, and caution is advised in individuals with renal impairment.

Adverse effects such as hypersensitivity reactions and nephrogenic systemic fibrosis (NSF) may occur, although the risk appears lower than in some other GBCAs. Proper patient evaluation and monitoring are essential during the administration of gadofosveset to ensure its safe and effective use. 

Pharmacodynamics: 

Mechanism of action: The mechanism of action of gadofosveset involves its ability to alter the magnetic properties of blood, leading to enhanced contrast in magnetic resonance imaging (MRI) scans.  

• Magnetic Properties: gadofosveset contains gadolinium, a paramagnetic element. Paramagnetic substances have unpaired electrons that create a magnetic field, which can influence the behavior of protons in the surrounding environment. 
• Interaction with Protons: In an MRI, protons in the body, particularly those in water molecules, act as tiny magnets. When a magnetic field is applied during imaging, the protons align themselves with the field. 
• Relaxation Effects: gadofosveset shortens nearby water protons’ relaxation times. It reduces the time it takes for the protons to return to their original alignment after being subjected to the magnetic field. 
• Contrast Enhancement: By accelerating the relaxation of nearby protons, gadofosveset enhances the contrast between blood vessels and surrounding tissues in MRI images. This increased contrast enables better visualization and differentiation of blood vessels, aiding in detecting and characterizing various vascular conditions. 
• Albumin Binding: gadofosveset has a unique characteristic of binding to serum albumin, a protein found in the blood. This binding allows gadofosveset to remain in the bloodstream for longer, extending the imaging window and providing sustained contrast enhancement during the imaging procedure. 

Pharmacokinetics: 

Absorption 

gadofosveset is administered intravenously, resulting in immediate and complete systemic availability. Upon injection, it rapidly enters the bloodstream and is distributed throughout the body. 

Distribution 

gadofosveset distributes in the extracellular space and has a relatively high protein binding affinity, specifically to albumin. This binding extends its half-life in the bloodstream and allows for a longer imaging window than other gadolinium-based contrast agents (GBCAs). gadofosveset does not readily cross the blood-brain barrier, which limits its distribution to the central nervous system. 

Metabolism 

gadofosveset is not significantly metabolized in the body. It remains intact, retaining its gadolinium chelate structure throughout its elimination process. 

Elimination and Excretion 

gadofosveset is primarily eliminated via renal excretion. The glomeruli in the kidneys filter it and subsequently excrete it in the urine. Due to its high protein binding, the excretion rate is slower than other GBCAs. The elimination half-life of gadofosveset is prolonged, allowing for an extended imaging time window. In patients with impaired renal function, the excretion of gadofosveset may be slower, necessitating caution and appropriate dose adjustments. 

Adminstartion

Administration: 

Intravenous administration 

gadofosveset is administered intravenously for contrast-enhanced magnetic resonance imaging (MRI) procedures.  

• Preparation: Before administering gadofosveset, the healthcare professional will review the patient’s medical history, including any allergies, kidney function, and other relevant factors. They will explain the procedure and address any questions or concerns the patient may have. 
• Intravenous Access: A suitable vein, typically in the arm, will be selected for intravenous access. The area may be cleaned with an antiseptic solution to reduce the risk of infection. 
• Injection: The gadofosveset contrast agent is provided in a pre-filled syringe. The healthcare professional will connect the syringe to the intravenous line and slowly inject the contrast agent into the vein. Depending on the specific instructions, the injection may take several seconds to a minute. 
• Observation: After the injection, the patient will be monitored for immediate adverse reactions or side effects. This observation period lasts a short duration, usually around 15 to 30 minutes. The healthcare professional will be vigilant for signs of allergic reactions or other complications. 
• Imaging Procedure: The patient will proceed with the MRI examination once the observation period is complete. The timing might vary depending on the specific imaging protocol and the area of the body being examined. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: gadofosveset 

Pronounced: (gad oh FOS ve set) 

Why do we use gadofosveset? 

gadofosveset is a gadolinium-based contrast agent (GBCA) used in magnetic resonance imaging (MRI) procedures to enhance the visibility and diagnostic capabilities of the images.  

• Vascular Imaging: gadofosveset is primarily used for vascular imaging, specifically to evaluate blood vessels and assess abnormalities in the cardiovascular system. It provides detailed visualization of arteries, veins, and capillaries, aiding in diagnosing and characterizing various vascular conditions. 
• Arterial Stenosis: gadofosveset-enhanced MRI can help identify and evaluate arterial stenosis, which refers to the narrowing of arteries due to plaque buildup or other causes. By enhancing the contrast between the blood vessel lumen and the surrounding tissues, gadofosveset assists in determining the severity and location of arterial stenosis. 
• Aneurysm Detection: gadofosveset helps detect and evaluate aneurysms, abnormal bulges, or weakened areas in blood vessels. By enhancing the contrast between the aneurysm sac and the surrounding structures, gadofosveset aids in assessing aneurysm size, shape, and location. 
• Arteriovenous Malformations (AVMs): gadofosveset-enhanced MRI plays a role in diagnosing and characterizing arteriovenous malformations, which are abnormal connections between arteries and veins. By providing detailed imaging of the abnormal blood vessels, gadofosveset assists in determining AVMs’ size, location, and complexity. 
• Tumors involving Blood Vessels: gadofosveset can help visualize and characterize tumors that involve blood vessels, such as vascular tumors or tumors with vascular involvement. It aids in assessing tumor vascularity, extent, and relationship with adjacent structures.