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[摘要]：NGR-hTNF is a vascular targeting agent that consists of a modified form of human TNF-alpha fused with an NGR peptide. The NGR peptide moiety of the compound acts by selectively targeting blood vessels, where TNF is released, resulting in the destruction of the tumor's blood supply and subsequent reduction in the size of the tumor. The NGR-mediated targeted delivery of TNF overcomes toxicity associated with systemic delivery of the agent. The compound has demonstrated good tolerability and promising antitumor activity in several phase I and II clinical studies in patients with a wide range of advanced/metastatic solid tumors, including malignant pleural mesothelioma, colorectal and hepatocellular carcinoma, as well as non-small cell lung cancer (NSCLC), administered either as monotherapy or in combination with chemotherapeutic regimens. NGR-hTNF is currently in phase Ill clinical development for the treatment of advanced malignant pleural mesothelioma. |
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