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Mitaplatin (ASK0912) is a platinum(IV) prodrug designed to co-deliver cisplatin and dichloroacetate (DCA) to cancer cells. Developed by Jiangsu Aosaikang Pharmaceutical, it aims to overcome platinum resistance and enhance efficacy by simultaneously targeting nuclear DNA and mitochondrial metabolism. Upon intracellular reduction, mitaplatin releases cisplatin, which induces DNA damage and apoptosis, and DCA, which inhibits pyruvate dehydrogenase kinase (PDK). Inhibition of PDK reverses the Warburg effect (aerobic glycolysis) in tumor cells, promoting mitochondrial oxidative phosphorylation and sensitizing cells to apoptosis. It has been primarily investigated in China for the treatment of unresectable hepatocellular carcinoma (HCC) as part of transarterial chemoembolization (TACE) regimens.
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