[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
Abstract Background Despite recent therapeutic advances, managing liver cancer remains a significant medical and economic priority for many countries. Patients often present at an advanced stage, preventing them from benefiting from salvage surgery. Consequently, palliative treatments play a crucial...
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SpringerOpen
2025-06-01
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| Series: | EJNMMI Radiopharmacy and Chemistry |
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| Online Access: | https://doi.org/10.1186/s41181-025-00352-9 |
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| author | Olivier Fougère Anne Dencausse Nicolas Lepareur Gaetan Van Simaeys Gilles Doumont Isabelle Gardin Elisabeth Renard Claire Hollenbeck Coraline De Maeseneire Nicolas Passon Olivier Rousseaux Sarah Catoen |
| author_facet | Olivier Fougère Anne Dencausse Nicolas Lepareur Gaetan Van Simaeys Gilles Doumont Isabelle Gardin Elisabeth Renard Claire Hollenbeck Coraline De Maeseneire Nicolas Passon Olivier Rousseaux Sarah Catoen |
| author_sort | Olivier Fougère |
| collection | DOAJ |
| description | Abstract Background Despite recent therapeutic advances, managing liver cancer remains a significant medical and economic priority for many countries. Patients often present at an advanced stage, preventing them from benefiting from salvage surgery. Consequently, palliative treatments play a crucial role in managing these cancers. Interventional radiology techniques are well-known for providing significant benefits to patients. [90Y]Y-L4-Lipo/Lipiodol® Ultra-Fluid is a novel transarterial radioembolization formulation designed for selective arterial injection to deliver localized radiation treatment of advanced unresectable liver tumors. This study aimed to confirm the stability of [90Y]Y-L4-Lipo/Lipiodol® Ultra-Fluid, investigate its biodistribution in an animal model, and conduct an initial dosimetry evaluation. Results Less than 3% of 90Y was released from the [90Y]Y-L4-Lipo/Lipiodol® Ultra-Fluid formulation in human serum. The tumor-to-liver activity ratio (T/NT) expressed in %ID/g tissue at 1 h, 24 h, 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 tumor tissue compared to healthy liver tissue. The extrapolated absorbed doses in Gy in humans to the tumor, normal liver, lung, and red marrow per GBq of [90Y]Y-L4-Lipo/Lipiodol® Ultra-Fluid administered were 54.3, 16.2, 0.69 and 0.89, for males, and 54.3, 22.3, 0.84 and 0.89, respectively, for females. Conclusion With good in vitro stability at low activity lasting at least 3 half-lives and a T/NT ratio of 4 in vivo, [90Y]Y-L4-Lipo/Lipiodol® Ultra-Fluid is confirmed as a valid candidate treatment for transarterial radioembolization of hepatocellular carcinoma. High activity stability in both in vitro and in vivo studies is needed to complete the formulation’s safety profile. |
| format | Article |
| id | doaj-art-e9a68c1069494c949b6edd2b535cd8b7 |
| institution | DOAJ |
| issn | 2365-421X |
| language | English |
| publishDate | 2025-06-01 |
| publisher | SpringerOpen |
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| series | EJNMMI Radiopharmacy and Chemistry |
| spelling | doaj-art-e9a68c1069494c949b6edd2b535cd8b72025-08-20T02:39:44ZengSpringerOpenEJNMMI Radiopharmacy and Chemistry2365-421X2025-06-0110111610.1186/s41181-025-00352-9[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 safetyOlivier Fougère0Anne Dencausse1Nicolas Lepareur2Gaetan Van Simaeys3Gilles Doumont4Isabelle Gardin5Elisabeth Renard6Claire Hollenbeck7Coraline De Maeseneire8Nicolas Passon9Olivier Rousseaux10Sarah Catoen11Research and Innovation DepartmentResearch and Innovation DepartmentUniv Rennes, Centre Eugène Marquis, Inserm, Inrae, Institut NUMECAN [(Nutrition, Métabolismes et Cancer)] - UMR_A 1341, UMR_S 1317Center for Microscopy and Molecular Imaging, Université Libre de BruxellesCenter for Microscopy and Molecular Imaging, Université Libre de BruxellesDepartment of Nuclear Medicine, Centre Henri BecquerelResearch and Innovation DepartmentResearch and Innovation DepartmentCenter for Microscopy and Molecular Imaging, Université Libre de BruxellesCenter for Microscopy and Molecular Imaging, Université Libre de BruxellesResearch and Innovation DepartmentResearch and Innovation DepartmentAbstract Background Despite recent therapeutic advances, managing liver cancer remains a significant medical and economic priority for many countries. Patients often present at an advanced stage, preventing them from benefiting from salvage surgery. Consequently, palliative treatments play a crucial role in managing these cancers. Interventional radiology techniques are well-known for providing significant benefits to patients. [90Y]Y-L4-Lipo/Lipiodol® Ultra-Fluid is a novel transarterial radioembolization formulation designed for selective arterial injection to deliver localized radiation treatment of advanced unresectable liver tumors. This study aimed to confirm the stability of [90Y]Y-L4-Lipo/Lipiodol® Ultra-Fluid, investigate its biodistribution in an animal model, and conduct an initial dosimetry evaluation. Results Less than 3% of 90Y was released from the [90Y]Y-L4-Lipo/Lipiodol® Ultra-Fluid formulation in human serum. The tumor-to-liver activity ratio (T/NT) expressed in %ID/g tissue at 1 h, 24 h, 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 tumor tissue compared to healthy liver tissue. The extrapolated absorbed doses in Gy in humans to the tumor, normal liver, lung, and red marrow per GBq of [90Y]Y-L4-Lipo/Lipiodol® Ultra-Fluid administered were 54.3, 16.2, 0.69 and 0.89, for males, and 54.3, 22.3, 0.84 and 0.89, respectively, for females. Conclusion With good in vitro stability at low activity lasting at least 3 half-lives and a T/NT ratio of 4 in vivo, [90Y]Y-L4-Lipo/Lipiodol® Ultra-Fluid is confirmed as a valid candidate treatment for transarterial radioembolization of hepatocellular carcinoma. High activity stability in both in vitro and in vivo studies is needed to complete the formulation’s safety profile.https://doi.org/10.1186/s41181-025-00352-9Hepatocellular carcinoma (HCC)Lipiodol® Ultra-FluidTransarterial radioembolization (TARE)Yttrium-90 |
| spellingShingle | Olivier Fougère Anne Dencausse Nicolas Lepareur Gaetan Van Simaeys Gilles Doumont Isabelle Gardin Elisabeth Renard Claire Hollenbeck Coraline De Maeseneire Nicolas Passon Olivier Rousseaux Sarah Catoen [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 EJNMMI Radiopharmacy and Chemistry Hepatocellular carcinoma (HCC) Lipiodol® Ultra-Fluid Transarterial radioembolization (TARE) Yttrium-90 |
| title | [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 |
| title_full | [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 |
| title_fullStr | [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 |
| title_full_unstemmed | [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 |
| title_short | [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 |
| title_sort | 90y y l4 lipo ethyl esters of iodized fatty acids of poppy seed oil lipiodol r ultra fluid a new tare formulation designed from a lipophilic ligand for stability and safety |
| topic | Hepatocellular carcinoma (HCC) Lipiodol® Ultra-Fluid Transarterial radioembolization (TARE) Yttrium-90 |
| url | https://doi.org/10.1186/s41181-025-00352-9 |
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