Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 52, Issue 22, Pages 6958-6961Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm901181h
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The design, synthesis, and biological characterization of an orally active prodrug (3) of gemcitabine are described. Additionally, the identification of a novel co-crystal solid form of the compound is presented. Valproate amide 3 is orally bioavailable and releases gemcitabine into the systemic circulation after passing through the intestinal mucosa. The compound has entered clinical trials and is being evaluated as a potential new anticancer agent.
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