Synthesis and Preclinical Evaluation of Radiolabeled [103Ru]BOLD-100

Barbara Happl, Marie Brandt, Theresa Balber, Katarína Benčurová, Zeynep Talip, Alexander Voegele, Petra Heffeter, Wolfgang Kandioller, Nicholas P. Van der Meulen, Markus Mitterhauser (Korresp. Autor*in), Marcus Hacker, Bernhard K. Keppler, Thomas L. Mindt (Korresp. Autor*in)

Veröffentlichungen: Beitrag in FachzeitschriftArtikelPeer Reviewed

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.

OriginalspracheEnglisch
Aufsatznummer2626
FachzeitschriftPharmaceutics
Jahrgang15
Ausgabenummer11
DOIs
PublikationsstatusVeröffentlicht - Nov. 2023

ÖFOS 2012

  • 301207 Pharmazeutische Chemie
  • 104003 Anorganische Chemie
  • 301904 Krebsforschung

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