Second generation pyridopyrazine-urea derivative compound series show highly selective PI3K-inhibition which could be valuable for cancer treatment
QUBEC CITY, Canada, April 16, 2007 terna Zentaris Inc. (TSX: AEZ; Nasdaq: AEZS), a global, pure play biopharmaceutical company focused on endocrine therapy and oncology, today presented an abstract outlining first in vitro data on its pyridopyrazine derivatives with high selectivity for PI3K inhibition, at the American Association for Cancer Research (AACR) Annual Meeting being held this week at the Los Angeles Convention Center in Los Angeles, California.
The poster #2379 entitled, New Generation of Anilino-Substituted Pyridopyrazine-Urea Derivatives Show Highly Selective PI3K-Inhibition, reviewed for the first time, results for a preclinical development program on a new generation of pyridopyrazine derivatives which clearly indicate that these drug candidates selectively inhibit PI3K.
Furthermore, an optimization process of our already known aryl-pyridopyrazine series led to the identification of a new lead compound in this series. A medicinal chemistry program was then initiated which resulted in the synthesis of new anilino-substituted pyridopyrazines. Out of this second generation series, several derivatives also with highly-selective PI3K inhibition as well as improved cellular efficacy and better drug-like properties, were identified.
Novel low molecular weight kinase inhibitor
Excellent in vitro activity against PI3K
High selectivity against a panel of more than 50 kinases
Anti-proliferative efficacy in diverse tumor cell-lines
Promising bioavailability observed for lead compound
PI3K signalling network covers enormous therapeutic potential
We are pleased with these results which exemplify our capability of developing novel therapeutic approaches that add to the breadth and depth of our product pipeline, said Dr Jrgen Engel, Executive Vice President, Global R&D and Chief Operating Officer at terna Zentaris. The potential for cancer treatment with agents inhibiting the PI3K pathway has become a focus in recent drug discovery and development research. We believe that by developing novel selective PI3K inhibiting small molecular compounds, we are positioning ourselves as one of the leaders in this promising therapeutic approach.
Cellular substrate phosphorylation studies targeting the inhibition of PI3K and functional cellular assays of tumor cell proliferation have been performed. In addition, physicochemical and initial ADMET data were collected. Several derivatives are currently undergoing first pharmacokinetic in vivo studies.
About terna Zentaris Inc.
terna Zentaris Inc. is a global, pure play biopharmaceutical company focused on endocrine therapy and oncology with proven expertise in drug discovery, development and commercialization.
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