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Gemin X Presents Mechanism of Action of GMX1778 and Preclinical Data of its Prodrug GMX1777-Data Discussed at the AACR-NCI-EORTC Conference on Molecular Targets and Cancer Therapeutics-Montréal, QC and Malvern, PA - October 24, 2007 - Gemin X Pharmaceuticals, Inc. announced the discovery of the mechanism of action of GMX1777 (EB1627), a soluble intravenously administered prodrug of the pharmacologically active compound GMX1778 (CHS828), and presented the results of preclinical data that lead to the design of the current first Phase 1 clinical trial of GMX1777. Data were presented in two poster sessions at the American Association of Cancer Research-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics in San Francisco. The study on the mechanism of action of GMX1777 was highlighted yesterday, October 23, 2007, in a poster presentation of an abstract titled,"GMX1777: A novel inhibitor of NAD+ biosynthesis via inhibition of nicotinamide phosphoribosyl transferase." The mechanism of action of the compound was initially believed to involve inhibition of NF-κB, a transcriptional factor that plays a role in cancer cell survival. Gemin X has discovered that GMX1778 functions by inhibiting nicotinamide phosphoribosyl transferase (NAMPRT), an enzyme involved in the biosynthesis of oxidized nicotinamide adenine dinucleotide (NAD+), and that NF-κB inhibition occurs as a consequence of NAMPRT inhibition and NAD+ decline. "We are encouraged by the key discovery of the mechanism of action of our second compound to enter the clinic. Rationally targeting a key metabolic pathway essential for cancer cell growth, resulting in cancer cell death independently of the status of the p53 tumor suppressor, opens new opportunities for clinical development both as a single agent and in combination with other cancer therapeutics, " stated Dr. Gordon Shore, Chief Scientific Officer of Gemin X. At a simultaneous poster session, the preclinical data were presented from an abstract titled, "Preclinical evaluation of the NAMPRT inhibitor prodrug GMX1777." NAMPRT, a recognized anti-cancer target, is an essential enzyme for the synthesis of NAD+ and is up-regulated in cancers. In this study, researchers evaluated several models of tumors in mice administered intramuscularly with GMX1777 and, consistent with the GMX1778 mechanism of action, observed that NAD+ levels decreased significantly prior to tumor regression. The data derived from the in vitro and in vivo studies suggest that GMX1777 exhibits mechanism-based efficacy against a wide range of human tumors and support the design of the first Phase 1 open-label, dose-escalation clinical trial on GMX1777 in patients with refractory solid tumors and lymphomas. About Gemin X |
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©2007 Gemin X Mentions Légales |
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