Preparation, characterization and evaluation of ¹⁸⁶Re‐idarubicin: a novel agent for diagnosis and treatment of hepatocellular carcinoma

Abstract

Hepatocellular carcinoma is a widely prevalent cancer, and hence, the development of radiopharmaceuticals for its management is an important issue. In the current investigation, the complexation of idarubicin with (186) Re was studied. Optimum labelling conditions were found to be 4 mg idarubicin, 1.5 mg stannous chloride dihydrate and ~70 MBq Re-186 at pH 7. The complex showed ~97.6% RCY value at 20 min and remained stable up to 24 h in the presence of 2.5 mg ascorbic acid. Molecular docking was performed to evaluate the complex binding to its target DNA-human topoisomerase II complex. Result of the in vivo evaluation showed that the complex tends to preferentially localize in cancerous tissues. The in vitro cell growth inhibition assay showed that the effect of the (186) Re-idarubicin was stronger than the effect of cold idarubicin, which strongly suggested that its cytotoxicity was mainly because of radiotoxicity rather than chemotherapeutic activity.

Radioiodination and biological distribution of a new s‐triazine derivative for tumor uptake evaluation

“…The maximum T/NT ratio was 3.73 ± 0.2 at 4 hours post injection. This ratio was higher than recently developed agents such as 99m TcN‐MAG‐AMCPP (1.83 after 1 hour), 99m Tc‐DMSAme (2.49 at 2 hours), and 186 Re‐idarubicin(2.93 at 2 hours) . Also, it showed a comparable result to 99m Tc‐sunitinib (3.2 after 3 hours), 99m Tc(CO)3‐labeled chlorambucil analogue (3.2 after 3 hours) .…”

“…This ratio was higher than recently developed agents such as 99m TcN-MAG-AMCPP (1.83 after 1 hour), 23 99m Tc-DMSAme (2.49 at 2 hours), 24 and 186 Re-idarubicin(2.93 at 2 hours). 25 Also, it showed a comparable result to 99m Tc-sunitinib (3.2 after 3 hours), 26 99m Tc(CO)3-labeled chlorambucil analogue (3.2 after 3 hours). 27 In comparison with 99m Tc-paclitaxil, compound 2 reached the maximum T/NT ratio (3.73) only 4 hours post injection, while 99m Tc-pacilataxil reached the its maximum ratio 24 hours (6.83) post injection.…”

Preparation of 186Re-Cefixime as a Potential Diagnostic and Therapeutic Agent for Bacterial Infection

“…The amount of stannous chloride less or greater than 0.5mg, such as 0.01 or 3mg leads to the RCY of 186 Re-cefixime decreasing to 75.6±1.5 or 60±1.2%, respectively. The RCY of 186 Re-Cefixime decreased in the low amount of SnCl 2 that may be attributed to its insufficient concentration to reduce the rhenium (VII) (ReO 4 -) to lower oxidation states (El-Kawy & Talaat, 2016). While most of the ligand molecule was consumed in the formation of complex, the perhenate is reduced to insoluble rhenium (IV) ReO 2 .xH 2 O in the absence of ligand at the high concentration of stannous chloride (Azmi et al, 2013).…”

Protective effects of Vitis vinifera (grapes) and one of its biologically active constituents, resveratrol, against natural and chemical toxicities: A comprehensive review

“…Idarubicin, a derivative of daunorubicin and an antileukemic medication, is used for the therapy of breast and lymphomas cancers (El‐Kawy & Talaat, ). The findings of an investigation indicated that GSPE reduced growth inhibitory effects of idarubicin on Chang liver cells, as well as the number of apoptotic cells.…”