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Pharmacokinetics of a novel anticancer ruthenium complex (KP1019, FFC14A) in a phase I dose-escalation study
Abstract
A phase I and pharmacokinetic study was carried out with the new ruthenium complex indazolium trans-[tetrachlorobis(1H-indazole)ruthenate(III)] (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.
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Cited by
NKP-1339, the first ruthenium-based anticancer drug on the edge to clinical application
Trondl, R., Heffeter, P., Kowol, C. R., Jakupec, M. A., Berger, W., & Keppler, B. K. (2014) · Chem. Sci. · doi:10.1039/c3sc53243g · Cited by 675
Self-citationRecent developments in ruthenium anticancer drugs
Levina, A., Mitra, A., & Lay, P. A. (2009) · Metallomics · doi:10.1039/b904071d · Cited by 592
Ruthenium-based chemotherapeutics: are they ready for prime time?
Antonarakis, E. S., & Emadi, A. (2010) · Cancer Chemotherapy and Pharmacology · doi:10.1007/s00280-010-1293-1 · Cited by 489
Meier-Menches, S. M., Gerner, C., Berger, W., Hartinger, C. G., & Keppler, B. K. (2018) · Chemical Society Reviews · doi:10.1039/c7cs00332c · Cited by 425
Self-citationMetal Drugs and the Anticancer Immune Response
Englinger, B., Pirker, C., Heffeter, P., Terenzi, A., Kowol, C. R., Keppler, B. K., & Berger, W. (2019) · Chemical Reviews · doi:10.1021/acs.chemrev.8b00396 · Cited by 355
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Metadata
- Authors
- Lentz, F., Drescher, A., Lindauer, A., Henke, M., Hilger, R. A., Hartinger, C. G., Scheulen, M. E., Dittrich, C., Keppler, B. K., & Jaehde, U.
- Venue
- Anti-Cancer Drugs
- Published
- 2009-02
- Volume
- 20
- Issue
- 2
- Pages
- 97-103
- ISSN
- 0959-4973 (ISSN-L)
- OpenAlex
- W2140928624
- Cited by
- 239
- References
- 0
- FWCI
- 4.77
- Type
- journal article
- Language
- en
- Open access
- closed
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- Lentz, F., Drescher, A., Lindauer, A., Henke, M., Hilger, R. A., Hartinger, C. G., Scheulen, M. E., Dittrich, C., Keppler, B. K., & Jaehde, U. (2009). Pharmacokinetics of a novel anticancer ruthenium complex (KP1019, FFC14A) in a phase I dose-escalation study. Anti-Cancer Drugs. https://doi.org/10.1097/cad.0b013e328322fbc5
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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