
Astex is a pioneer in fragment-based drug discovery.
We use our proprietary drug discovery platform Pyramid™ to efficiently and rapidly identify and characterize novel small molecule drugs.
We are developing new targeted therapies for patients with advanced cancer that are designed to be more effective and less toxic than current treatments
Astex has a broad and expanding pipeline of products in clinical and preclinical development all of which have been generated internally using its proprietary drug discovery engine, Pyramid™.
AT7519 is Astex's most progressed drug candidate which entered Phase I clinical trials mid 2005. AT7519 is a potent cell cycle inhibitor that targets key cyclin-dependent kinases resulting in tumour shrinkage. Further Phase I and Phase I/IIa clinical studies of AT7519 in patients with solid tumours and haematological malignancies respectively commenced in Q4 2006 and Q1 2007.
Astex's second clinical-stage compound, AT9283 entered into a phase I/IIa clinical study in patients with hematological malignancies in the US in Q3 2006, and in patients with solid tunours in two separate studies at centres in the UK and in Canada in Q42006 and Q1 2007. AT9283 is a potent inhibitor of aurora kinases A and B, JAK2 and abl kinases and has been shown to arrest tumour growth. The aurora kinases play a key role in mitotic checkpoint control in cell division and are over-expressed in many human tumours. JAK2 activity has recently been identified as a key driver of several haematological malignancies and as such its inhibition has considerable potential in the treatment in a spectrum of diseases.T he Company has two further clinical candidates; AT9311, a selective, orally active, cell cycle inhibitor and AT13387, a non-ansamycin inhibitor of Hsp90, both of which are in formal pre-clinical development. All four of Astex's current drug products have been discovered internally using the Company's proprietary drug discovery approach.
Astex's leading position in fragment-based drug discovery derives from its integrated discovery engine, Pyramid™. Pyramid™ combines novel and proprietary small molecule fragment libraries with computational chemistry and structural biology using biophysical techniques including X-ray crystallography and NMR spectroscopy to identify drug fragments bound to target proteins. These fragments are then rapidly transformed using efficient medicinal chemistry into potent, selective lead compounds.
By careful monitoring of key characteristics such as ligand efficiency and in vivo activity during lead optimization, Astex's fragment based drug discovery approach ensures delivery of potent, selective and low molecular weight compounds with optimised drug metabolism and pharmacokinetic properties, thus reducing attrition during clinical development. Pyramid™ has been successfully applied by Astex across a wide variety of therapeutic targets, including those regarded as 'intractable' by the pharmaceutical industry, resulting in lead compounds for the potential treatment of cancer, inflammation and Alzheimer's disease.
Pyramid™ has been successfully applied across a wide variety of therapeutic targets, including those regarded as 'intractable' by the pharmaceutical industry, resulting in lead compounds for the potential treatment of cancer, inflammation and Alzheimer's disease.
Astex was established in 1999 and is well financed by leading, blue chip US and European investors (Abingworth, Advent International, Alta Partners, Apax, GIMV, HypoVereinsbank, Oxford Bioscience Partners, Schering AG and the University of Cambridge).
For further information on Astex please visit the Company's website at www.astex-therapeutics.com
Astex plans to partner its products at an appropriate stage of clinical development while retaining significant commercialization rights from its partnerships.
Astex's unprecedented productivity in lead discovery has been endorsed by drug discovery collaborations with leading pharmaceutical company partners including Astellas Pharma, AstraZeneca, Boehringer Ingelheim, Mitsubishi Pharma, Novartis, sanofi-aventis and Schering. These partnerships have validated Astex's technology and provide a revenue stream, in the form of upfront fees, research and development funding, milestones and royalties, to fund Astex's internal research.