Approved Blood Pool Agents: First-Pass Imaging

The key differentiating characteristic of gadofosveset is its reversible binding to human serum albumin (HSA) after distribution.
The presence of gadolinium results in a shortening of the longitudinal relaxation time of neighbouring protons and thus generates positive enhancement of the blood pool in T1-weighted images. (Gadofosveset has no effect on T2-weighted images at clinical doses).
Compared to other available MRI agents, the protein binding of gadofosveset provides increased vascular enhancement by remaining in the blood for several hours.
The T1 relaxivity rate of gadofosveset at 1.5 T is 5 times higher than the relaxivity of standard gadolinium contrast agents.
Gadofosveset can be used for conventional dynamic MRA scans (first-pass) as well as high-resolution (steady-state) depiction of multiple vascular regions for approximately one hour following a single administration.

After i.v. injection, a fraction of approx. 85% of gadofosveset is bound to human serum albumin. The strongest binding of gadofosveset to albumin and the greatest increase in relaxivity have been observed in human plasma. (Slightly different rates exist for different species.)
The safety and tolerability of gadofosveset has been extensively investigated in clinical trials with doses up to 0.15 mmol/kg body weight, which equals five times the recommended clinical dose.
Results of various evaluations of plasma and urine samples indicate that gadofosveset does not undergo measurable metabolism in humans or laboratory animals.
Gadofosveset is excreted mainly in the urine, a small amount also being detectable in the faeces.
In-vitro studies failed to reveal any evidence of drug-drug interactions. There was no detectable displacement of warfarin, ibuprofen, digitoxin, propranolol, verapamil from 4.5% human serum albumin and it was thus concluded that gadofosveset does not adversely interact with those substances or with phenprocoumon, diazepam, ketoprofen, naproxen, diclofenac or piroxicam at clinically relevant doses.
The relaxation rate (1/T1) of gadofosveset was not affected by these drugs at therapeutic relevant doses.

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