Pharmacokinetics of a novel anticancer ruthenium complex (KP1019, FFC14A) in a phase i dose-escalation study

Author(s)
Frederike Lentz, Anne Drescher, Andreas Lindauer, Magdalena Henke, Ralf A. Hilger, Christian Hartinger, Max E. Scheulen, Christian Dittrich, Bernhard Keppler, Ulrich Jaehde
Abstract

A phase I and pharmacokinetic study was carried out with the new ruthenium complex indazolium trans-[tetrachlorobis(1 H-indazole)ruthenate(lll)] (KP1019, FFC14A). Seven patients with various types of solid tumours refractory to standard therapy were treated with escalating doses of KP1019 (25-600 mg) twice weekly for 3 weeks. No dose-limiting toxicity occurred. Ruthenium plasma concentration-time profiles after the first dose and under multiple-dose conditions were analysed using a compartmental approach. The pharmacokinetic disposition was characterised by a small volume of distribution, low clearance and long half-life. Only a small fraction of ruthenium was excreted renally. The area under the curve values increased proportionally with dose indicating linear pharmacokinetics.

Organisation(s)
Department of Inorganic Chemistry
External organisation(s)
Rheinische Friedrich-Wilhelms-Universität Bonn, Universität Duisburg-Essen, Sozialmedizinisches Zentrum Süd – Kaiser-Franz-Josef-Spital
Journal
ANTI-CANCER DRUGS
Volume
20
Pages
97-103
No. of pages
7
ISSN
0959-4973
DOI
https://doi.org/10.1097/CAD.0b013e328322fbc5
Publication date
2009
Peer reviewed
Yes
Austrian Fields of Science 2012
104003 Inorganic chemistry, 301305 Medical chemistry
Portal url
https://ucrisportal.univie.ac.at/en/publications/b17218c2-3832-4930-9dae-90ff4dac5621