SALT LAKE CITY, Nov. 17, 2010 (GLOBE NEWSWIRE) -- Myrexis, Inc. (Nasdaq:MYRX), a biotechnology company focused on discovering, developing, and commercializing novel treatments for cancer, today presented two posters at the 22nd European Organisation for Research and Treatment of Cancer (EORTC), National Cancer Institute (NCI) and American Association for Cancer Research (AACR) Symposium on "Molecular Targets and Cancer Therapeutics," in Berlin, Germany. The presentations further demonstrate best-in-class potential for the Company's cancer metabolism inhibitor, MPC-9528, which has previously been shown to cause profound and durable tumor regressions across multiple tumor types.
MPC-9528 exhibited superior potency in enzymatic, cellular, and mouse xenograft models, compared to other small molecules that target the same metabolic enzyme. Furthermore, MPC-9528 demonstrated synergy with poly(ADP-ribose) polymerase (PARP) inhibitors, which are involved in DNA repair and are active against tumors with genetic deficiency for BRCA.
"Based upon the data we've collected to date, we remain confident in the best-in-class profile of our cancer metabolism inhibitor," said Robert Carlson, Ph.D., Vice President and Head of Research at Myrexis. "We are encouraged by the superior potency, therapeutic index and potential for broad therapeutic application of our compound. We are also excited about the opportunities for combination of MPC-9528 with other chemotherapeutics to achieve synergistic anti-tumor activity."MPC-9528 inhibits cancer metabolism by targeting nicotinamide phosphoribosyltransferase, or Nampt, a key enzyme in the primary pathway for producing nicotinamide adenine dinucleotide (NAD), which is required by all cells to carry out normal functions such as glucose metabolism, DNA repair and gene expression. By exploiting cancer cells' increased requirements for NAD, MPC-9528 is able to selectively inhibit the growth of tumor cells. In a poster titled, "Anti-Tumor Activity of MPC-9528, GMX1778 and APO866: Nampt Inhibitors of Three Different Structural Classes," Myrexis showed that MPC-9528 was the most potent inhibitor of human Nampt and caused the most efficient NAD depletion and cell death in cancer cell lines in vitro. In addition, MPC-9528 also demonstrated the greatest in vivo potency in pre-clinical models. Myrexis also presented a poster titled, "The Nampt Inhibitor MPC-9528 and the PARP Inhibitor Olaparib Synergize in Killing BRCA-Deficient Cancer Cell Lines." The Company demonstrated that MPC-9528 and oliparib inhibit PARP by distinct mechanisms, and as a result, are strongly synergistic against BRCA1 (-/-) and BRCA2 (-/-) cancer cell lines. Specifically, sub-lethal doses of MPC-9528 enhanced the potency of olaparib in a BRCA-dependent manner.