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Comparative protein binding, stability and degradation of Satraplatin, JM118 and Cisplatin in human plasma in vitro


Bell, DN and Liu, JJ and Tingle, MD and Rattel, B and Meyer, TU and McKeage, MJ, Comparative protein binding, stability and degradation of Satraplatin, JM118 and Cisplatin in human plasma in vitro, Clinical and Experimental Pharmacology and Physiology, 35 pp. 1440-1446. ISSN 0305-1870 (2008) [Refereed Article]

Copyright Statement

Copyright 2008 The Authors Journal compilation Copyright 2008 Blackwell Publishing Asia Pty Ltd

DOI: doi:10.1111/j.1440-1681.2008.05017.x


1. Satraplatin is an investigational orally administered platinum-based antitumour drug. The present study compared the plasma protein binding, stability and degradation of satraplatin with that of its active metabolite JM118 and cisplatin. 2. The platinum complexes were incubated in human plasma for up to 2 h at 37°C and quantified in plasma fractions by inductively coupled plasma–mass spectrometry on- or off-line to high-performance liquid chromatography. 3. All three platinum drugs became irreversibly bound to plasma proteins and showed negligible reversible protein binding. They were also unstable in plasma and generated one or more platinum-containing degradation products during their incubation. However, the three platinum complexes differed in the kinetics of their instability and protein binding, as well as in the number of degradation products formed during their incubation. 4. In conclusion, the plasma protein binding, instability and degradation of satraplatin and its active metabolite JM118 are qualitatively similar to that of cisplatin and other clinically approved platinum-based drugs. Quantitative differences in their irreversible protein binding and degradation were related to their respective physiochemical properties and bioactivation mechanisms. Key words: cancer chemotherapy, cisplatin, HPLC–ICP–MS, JM216, plasma stability, platinum-based drugs, protein binding, satraplatin.

Item Details

Item Type:Refereed Article
Keywords:satraplatin, cisplatin, protein binding, stability
Research Division:Biomedical and Clinical Sciences
Research Group:Pharmacology and pharmaceutical sciences
Research Field:Clinical pharmacology and therapeutics
Objective Division:Health
Objective Group:Clinical health
Objective Field:Clinical health not elsewhere classified
UTAS Author:Liu, JJ (Dr Johnson Liu)
ID Code:89123
Year Published:2008
Web of Science® Times Cited:19
Deposited By:Pharmacy
Deposited On:2014-02-25
Last Modified:2017-01-09

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