An update on satraplatin: the first orally available platinum anticancer drug

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Abstract
This update focuses on the clinical development of the first orally available platinum-containing anticancer drug, satraplatin (JM216, BMS 182751, BMY 45594). Satraplatin was selected for clinical study on the basis of possessing several promising preclinical features the first of which is it’s potent in vitro growth inhibitory properties against several tumour types (mean IC50 approximately equals 1 μM). Secondly, it possesses in vivo oral antitumour activity against a variety of murine and human sc. tumour models, broadly comparable to the level of activity obtainable with parenterally administered cisplatin or carboplatin. Lastly, it has a relatively mild toxicity profile with myelosuppression being dose-limiting. Satraplatin entered clinical trials in 1992 and is now undergoing Phase III evaluation. Non-linear pharmacokinetics, probably due to saturable absorption, was observed when the drug was administered as a bolus every 3 - 4 weeks. Subsequent Phase II trials have used a daily schedule for five c...

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