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[摘要]：Since cancer cells do not produce blood vessels, tumors usually contain regions of hypoxia with relatively low metabolic activity and regions with relatively normal oxygenation where cancer cells grow much more rapidly. Most current cytotoxic anticancer drugs inhibit the growth of highly metabolic cancer cells, while not affecting the hypoxic cancer cells, which remain to grow more aggressively following chemotherapy. TH-302 is a phosphoramidate-based prodrug which becomes activated by electron reduction involving NADPH cytochrome P450 or other reductases present in hypoxic tumor tissue. Preclinical studies have demonstrated the unique hypoxic specificity and therapeutic efficacy of TH-302 in a variety of common human cancer cells. The results of phase I and II clinical trials indicate that this compound has clinical promise in terms of pharmacokinetics, safety and effectiveness for the treatment of various solid tumors in human cancer patients. |
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