Title
Synthesis and Preclinical Evaluation of Radiolabeled [103Ru]BOLD-100
Author
Marie Brandt
Ludwig Boltzmann Institute Applied Diagnostics, General Hospital of Vienna
Author
Theresa Balber
Ludwig Boltzmann Institute Applied Diagnostics, General Hospital of Vienna
... show all
Abstract
The first-in-class ruthenium-based chemotherapeutic agent BOLD-100 (formerly IT-139, NKP-1339, KP1339) is currently the subject of clinical evaluation for the treatment of gastric, pancreatic, colorectal and bile duct cancer. A radiolabeled version of the compound could present a helpful diagnostic tool. Thus, this study investigated the pharmacokinetics of BOLD-100 in more detail to facilitate the stratification of patients for the therapy. The synthesis of [103Ru]BOLD-100, radiolabeled with carrier added (c.a.) ruthenium-103, was established and the product was characterized by HPLC and UV/Vis spectroscopy. In order to compare the radiolabeled and non-radioactive versions of BOLD-100, both complexes were fully evaluated in vitro and in vivo. The cytotoxicity of the compounds was determined in two colon carcinoma cell lines (HCT116 and CT26) and biodistribution studies were performed in Balb/c mice bearing CT26 allografts over a time period of 72 h post injection (p.i.). We report herein preclinical cytotoxicity and pharmacokinetic data for BOLD-100, which were found to be identical to those of its radiolabeled analog [103Ru]BOLD-100.
Keywords
ruthenium-103BOLD-100anti-cancer metallodrugsin vivo studiespharmacokinetics
Object type
Language
English [eng]
Persistent identifier
https://phaidra.univie.ac.at/o:2045439
Appeared in
Title
Pharmaceutics
Volume
15
Issue
11
ISSN
1999-4923
Issued
2023
Publisher
MDPI AG
Date issued
2023
Access rights
Rights statement
© 2023 by the authors
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