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

journal contribution
posted on 2023-05-17, 22:32 authored by Bell, DN, Johnson Liu, Tingle, MD, Rattel, B, Meyer, TU, McKeage, MJ
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.


Publication title

Clinical and Experimental Pharmacology and Physiology








School of Pharmacy and Pharmacology


Blackwell Publishing Asia

Place of publication

54 University St, P O Box 378, Carlton, Australia, Victoria, 3053

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

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Clinical health not elsewhere classified

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