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Norcantharidin Lipid Microsphere for Injection is an intravenous formulation of norcantharidin (NCTD), a synthetic demethylated derivative of cantharidin, developed by Beijing Nuokangda Pharmaceutical Technology. The drug is encapsulated within lipid microspheres—an oil-in-water emulsion system typically composed of soybean oil and lecithin—to enhance its solubility, improve bioavailability, and mitigate the severe nephrotoxicity and cardiotoxicity associated with traditional norcantharidin salts. Norcantharidin functions as a small molecule inhibitor of protein phosphatase 2A (PP2A), a key regulator of signaling pathways involved in cell growth and survival. By inhibiting PP2A, the drug induces G2/M phase cell cycle arrest and triggers apoptosis in malignant cells. This formulation is currently being evaluated in Phase I clinical trials for the treatment of locally advanced or metastatic solid tumors.
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