RESUMEN
Radioisotope-labelled lipiodol has been used in the therapy of liver cancer. Recently a lipiodol solution of 188Re-labelled diaminedithiol (DD) has been reported to show a high uptake in the liver cancer. We synthesized long-chain alkyl DD derivatives to improve their uptake and retention in tissue. As the length of the alkyl chain increased, tissue uptake and retention also increased due to hydrophobic interaction with lipiodol. Among the synthesized compounds, the lipiodol solution of 188Re-HDD, the DD derivative with the longest side chain (C16), is a promising agent for therapy of liver cancer.
Asunto(s)
Aceite Yodado/farmacocinética , Neoplasias Hepáticas/metabolismo , Compuestos Organometálicos/síntesis química , Compuestos Organometálicos/farmacocinética , Radiofármacos/síntesis química , Radiofármacos/farmacocinética , Animales , Humanos , Neoplasias Hepáticas/radioterapia , Pulmón/metabolismo , Ratones , Ratones Endogámicos ICR , Compuestos Organometálicos/uso terapéutico , Radiofármacos/uso terapéutico , Distribución TisularRESUMEN
INTRODUCTION: The aim of this study was to investigate the potential of using 188Re Lipiodol for selective internal radiation therapy of inoperable hepatocellular carcinoma (HCC). CLINICAL PICTURE: A 33-year-old female with poorly-differentiated multicentric HCC, elevated alpha-fetoprotein (AFP) and increased serum alkaline phosphatase. TREATMENT: Over a 2-month interval, the patient was treated twice with 4GBq of 188Re-TDD-Lipiodol. OUTCOMES: There was good localisation of 188Re Lipiodol in the tumours, but also in thyroid (first treatment) and gastrointestinal tract (both treatments). So far (5 months post-treatment), the patient remains well with stable disease. CONCLUSIONS: 188Re Lipiodol can be an effective radiopharmaceutical for the treatment of HCC; however, more work must be done to minimise the uptake in bowel.
Asunto(s)
Antineoplásicos/uso terapéutico , Carcinoma Hepatocelular/radioterapia , Aceite Yodado , Neoplasias Hepáticas/radioterapia , Compuestos Organometálicos/uso terapéutico , Radiofármacos/uso terapéutico , Adulto , Antineoplásicos/administración & dosificación , Femenino , Humanos , Compuestos Organometálicos/administración & dosificación , Radiofármacos/administración & dosificación , Dosificación RadioterapéuticaRESUMEN
Radiolabeled lipiodol has been used for targeting liver cancer. We developed a lipiodol solution of (188)Re-TDD (2,2,9,9-tetramethyl-4,7-diaza-1,10-decanedithiol) and investigated its feasibility for the treatment of liver cancer. The lipiodol solution of (188)Re-TDD was well-retained in the lipiodol phase in vitro. After injection through the tail veins of mice, high lung-uptake was investigated which is evidence of embolizing activity. We also found high accumulation in hepatoma after injection through the hepatic arteries of hepatoma-bearing rats. In conclusion, the lipiodol solution of (188)Re-TDD is a promising agent for liver cancer therapy.