Chemical formula: C₁₇H₂₉GdN₄O₇ Molecular mass: 558.68 g/mol PubChem compound: 60714
Gadoteridol is a non-ionic paramagnetic contrast medium for Magnetic Resonance Imaging.
When placed in a magnetic field, gadoteridol decreases T1 relaxation times in targeted areas. At recommended doses, the effect is observed with greatest sensitivity in the T1-weighted sequences.
However, disruption of the blood-brain barrier or normal vascularity allows penetration of gadoteridol into lesions such as neoplasms, abscesses, and subacute infarcts.
The pharmacokinetics of intravenously administered gadoteridol in normal subjects conforms to a two-compartment open model with mean distribution and elimination half-lives (reported as mean ± SD) of about 0.20 ± 10.04 hours and 1.57 ± 10.08 hours, respectively.
Gadoteridol is exclusively eliminated in the urine with 94.4 ± 4.8% (mean ± SD) of the dose excreted within 24 hours post injection. There is no detectable biotransformation or decomposition of gadoteridol.
The renal and plasma clearance rates (1.41 ± 0.33 ml/min/kg and 1.50 ± 0.35 ml/min/kg, respectively) of gadoteridol are essentially identical, indicating no alteration in elimination kinetics on passage through the kidneys and that the drug is essentially cleared through the kidney. The volume of distribution (204 ± 58 ml 1 kg) is equal to that of extra cellular water, and clearance is similar to that of substances which are subject to glomerular filtration.
No serum protein binding was detected in rats.
Preclinical data indicate no additional risks for humans based on conventional studies of safety pharmacology, repeated dose toxicity or genotoxicity. Carcinogenicity studies have not been conducted.
Reproduction toxicity studies gave no indication of teratogenic potential. Rats and rabbits thatreceived gadoteridol for 12-13 days during gestation showed an increase in post-implantation loss/abortion at doses 20-33 times the maximum human dose of 0.3mmol/kg/day. The offspring of rats treated at this dose also showed an increased spontaneous motor activity.
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