TopoTarget and CuraGen present encouraging new preclinical data on PXD101 at the AACR 97th Annual Meeting

TopoTarget A/S (CSE: TOPO) and CuraGen Corp. (Nasdaq: CRGN) announced yesterday encouraging new preclinical data on PXD101, their novel histone deacetylase (HDAC) inhibitor being investigated for the treatment of cancer.

Recent preclinical studies presented at the 97th Annual Meeting of the American Association for Cancer Research (AACR) in Washington, D.C., US have demonstrated that PXD101 potently inhibited the growth of numerous lung cancer cell lines in vitro and reduced the growth of lung cancer xenografts in vivo. When used in combination with erlotinib (Tarceva®), PXD101 displayed synergistic growth-inhibitory activity in vitro and caused greater tumour growth inhibition than did the respective monotherapies in animals harbouring human lung cancer xenografts. PXD101 decreased the expression of EGFR (Epidermal Growth Factor Receptor) family members EGFR and ErbB3, a finding which may help to explain the synergistic activity of PXD101 and erlotinib. PXD101 also demonstrated strong synergistic activity with pemetrexed (Alimta®), an effect potentially related to down-regulation of thymidylate synthase by PXD101.

Researchers from TopoTarget and CuraGen presented the results on Tuesday, April 4, 2006, in a poster entitled: “Activity of the HDAC Inhibitor, PXD101, in Preclinical Lung Cancer Studies”.

In a second poster presentation entitled, “Plasma and Cerebrospinal Fluid (CSF) Pharmacokinetics of the Histone Deacetylase (HDAC) Inhibitor, PXD101, in Non-Human Primates,” researchers from the National Cancer Institute, TopoTarget and CuraGen reported preclinical pharmacokinetic results. These results showed that PXD101 displayed a half-life of approximately one hour, with cerebrospinal fluid (CSF) penetration by PXD101 of approximately 1%. The results suggest that the concentration of PXD101 achieved in the CSF may be sufficient to inhibit the growth of certain cancers.

Peter Buhl Jensen, CEO in TopoTarget commented: “These preclinical studies continue to highlight the potential of PXD101, both as a single agent and in combination with other anti-cancer therapies. We are already evaluating PXD101 in multiple Phase II and Phase Ib/II clinical trials for the treatment of multiple myeloma, T-cell lymphomas, ovarian cancer and colorectal cancer. In addition, we anticipate the initiation of several NCI-sponsored clinical trials throughout 2006. We aim to report preliminary results from our PXD101 studies from mid-2006 and into 2007.”