Astex Drug Candidates to be Presented at the 2008 AACR Annual Meeting
Cambridge, UK, 8th April 2008
Cambridge, UK, 8th April 2008. Astex Therapeutics announced today that data on three of its drug candidates, AT7519, AT9283 and an FGFr kinase inhibitor, will be presented at the 2008 AACR Annual Conference, to be held April 12-16, 2008 in San Diego. All three drug candidates were discovered internally using Astex’s industry-leading fragment-based drug discovery platform, Pyramid™.
Dr. David Rees, Vice President Medicinal Chemistry, will be making Astex’s first public disclosure of the full chemical structure of AT7519 during his talk in the ‘Meet-the-Expert Session’. AT7519 is a potent cell cycle inhibitor that targets key cyclin-dependent kinases and is in Phase I studies in patients with solid tumours with additional Phase II studies planned for 2008.
In addition, Astex will present data which demonstrates the activity of its multi-targeted kinase inhibitor, AT9283, in Chronic Myelogenous Leukemia models, particularly cell lines and patient samples that are resistant to existing therapies such as Sprycel®, Tasigna® and Gleevec®. AT9283 is currently in Phase I trials in patients with solid tumours and Phase I/II trials in patients with leukaemias where early clinical activity has been observed.
Astex will also make the first disclosure of uniquely selective inhibitors of the Fibroblast Growth Factor Receptor (FGFr) kinase, which have shown potent antitumour activity in FGFr dependent xenograft models. The wide number of cancers that are associated with FGFr dependence include breast, colorectal, endometrial, bladder, multiple melanoma, prostate and angiogenesis.
Astex has a further five internal drug discovery programmes and is pursuing an additional five projects in partnership with leading pharmaceutical companies including Novartis, AstraZeneca, Bayer Schering and Boehringer Ingelheim.
Meet-the-Expert Session at the 2008 AACR Annual Meeting
Session Title: Fragment Based Drug Discovery
Session Date: Monday 14 April, 2008, 7:00 AM to 8:00 AM
Session Location: Room 11A-B
Poster Presentations at the 2008 AACR Annual Meeting
Poster Title: AT9283, a potent inhibitor of Bcr-Abl T315I, is active in CML models
Session Date: Monday, April 14, 2008, 1:00 PM
Session ID: Clinical Research 10
Permanent Abstract Number: 2820
Poster Title: Development of inhibitors of the fibroblast growth factor receptor (FGFr) kinase using a fragment based approach
Session Date: Sunday, April 13, 2008, 1:00 PM
Session ID: Experimental and Molecular Therapeutics 14
Permanent Abstract Number: 1545
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Contacts
Astex Therapeutics Limited
Romaine Miles
Corporate Communications
Email: r.miles@astex-therapeutics.com
Tel: +44 (0) 1223 226200
Web: www.astex-therapeutics.com
Notes to News Editors
AT7519
AT7519 is a targeted inhibitor of cyclin-dependent kinases (CDKs) which are involved in the regulation of the cell cycle and of gene expression, and their dysregulation is associated with the progression of certain malignancies. By inhibiting certain CDKs, we may be able to eliminate rapidly proliferating malignant cells. AT7519 is currently being investigated in two Phase I clinical trials as a treatment for solid tumours. AT7519 also has potential in the treatment of a broad range of solid tumours and other haematological malignancies such as chronic lymphocytic leukaemia (CLL), and we intend to establish additional Phase II trials to explore this potential following completion of the current Phase I trials.
AT9283
AT9283 is a multi-targeted inhibitor of the kinases Aurora A, Aurora B, BCR–Abl and JAK2. The over-expression or aberrant activation of each of these kinase targets is associated with the development and/or progression of different cancers. By inhibiting one or more of these kinases, we expect we may be able to affect the progression of diseases associated with their dysregulation. AT9283 is currently being investigated as monotherapy in three trials in patients with solid tumours and haematological malignancies. We are focusing our initial efforts on the development of AT9283 to treat elderly patients with acute myelogenous leukaemia (AML), patients with relapsed or refractory AML and patients with intermediate-high risk myelofibrosis (MF). Dependent on the results of our clinical trials, we may initiate additional clinical trials to explore the potential of AT9283 in the treatment of other haematological malignancies and solid tumours.
FGFr
FGFr is a receptor tyrosine kinase which activates the extracellular signal-regulated kinase / mitogen-activated protein kinase and the protein kinase B / Akt pathways which promote cell growth and survival. Amplification, over-expression or activating mutations of fibroblast growth factor receptor have been associated with multiple myeloma and with breast, prostate, colon, and bladder cancers. Astex’s FGFr programme is directed towards the identification of selective inhibitors of FGFrs suitable for oral chronic therapy. In particular, these agents are designed to avoid toxicities such as hypertension, fluid retention, and renal and cardiac impairment that have been reported following treatment with existing broad-spectrum inhibitors.
About Astex
Astex Therapeutics is a biotechnology company that discovers and develops novel small molecule therapeutics. Using its pioneering fragment-based drug discovery platform Pyramid™, Astex has built a pipeline of five molecularly-targeted oncology drugs, of which two are currently being tested in clinical trials, one has IND approval, and two are in pre-clinical development.
In addition to its proprietary research programmes, Astex’s productivity in lead discovery has been endorsed through numerous partnerships with major pharmaceutical companies, including Novartis, AstraZeneca, and Boehringer Ingelheim.
For further information on Astex Therapeutics please visit the Company’s website at www.astex-therapeutics.com