[90Y]Y-L4-Lipo/ Ethyl esters of iodized fatty acids of poppy seed oil (Lipiodol® Ultra-Fluid), a new TARE formulation, designed from a lipophilic ligand for stability and safety
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Background: Despite recent therapeutic advances, liver cancer management remains a medico-economic priority for several countries. Patients frequently present at an advanced stage, preventing them from benefiting from salvage surgery. Therefore, palliative treatments play an important role in the management of these cancers. Among them, interventional radiology techniques are well-known for bringing significant benefit to patients. [ 90 Y]Y-L4-Lipo/Lipiodol ® Ultra-Fluid is a new transarterial radioembolization formulation designed for delivery through selective arterial injection for local radiation treatment of advanced unresectable liver tumors. The objective of the presented study was to confirm the stability of [ 90 Y]Y-L4-Lipo/Lipiodol ® Ultra-Fluid, investigate its biodistribution in an animal model and obtain an initial dosimetry evaluation. Results: Less than 3% of 90 Y was released from [ 90 Y]Y-L4-Lipo/Lipiodol ® Ultra-Fluid in human serum. The ratio of tumor to non-tumoral liver activity (T/NT) expressed in %ID/g tissue at 1 hour, 24 hours, 3 days, and 6 days (5.50 ± 2.42, 3.28 ± 1.94, 4.89 ± 3.41 and 4.77 ± 1.59, respectively) suggests effective targeting of tumoral tissue compared to healthy liver tissue . The extrapolated absorbed doses Gy in humans to the tumor, normal liver, lung, and red marrow per GBq of [ 90 Y]Y-L4-Lipo/Lipiodol ® Ultra-Fluid administered were 54.3, 16.2, 0.69 and 0.89 respectively, for male, and 54.3, 22.3, 0.84 and 0.89 for female. Conclusion: With good in vitro stability at low activity lasting at least 3 half-lives and a T/NT ratio of 4 in vivo , [ 90 Y]Y-L4-Lipo/Lipiodol ® Ultra-Fluid is confirmed as a valid candidate treatment for transarterial radioembolization of hepatocellular carcinoma. High activity stability in in vitro and in vivo studies are needed to complete the safety profile of the formulation.
