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Nanoliposomal anti-cancer HIF-1メ inhibitor
RX-0047-Nano is a nanoliposomal cancer drug candidate that selectively inhibits expression of the HIF-1メ transcription factor. HIF-1メ is a key signaling molecule in angiogenesis, cancer cell survival and invasion, and radiation resistance. RX-0047 is a first-in-class anticancer candidate that directly inhibits expression of mRNA and protein of HIF-1メ.
HIF-1メ is over-expressed in a broad range of human cancers, and associated with increased cancer mortality and resistance.
In preclinical studies, RX-0047 significantly downregulated expression of HIF-1メ mRNA and protein. At nanomolar concentrations, RX-0047 reversed resistance in radiation-resistant cancer cells. RX-0047 inhibited growth of solid tumors in lung as well as prostate cancer xenograft models, and significantly blocked metastasis in a lung metastatic model. RX-0047-Nano is expected to provide significant clinical benefits including targeted higher cellular uptake, extended circulation time, reduced drug-related toxicity, and improved efficacy. Phase I trials are planned for 2009.
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