Pyramid™: Fragment Based Drug Discovery
Astex has established its integrated, fragment-based drug discovery approach, Pyramid™, as an industry-leading platform that rapidly delivers tailored, high-quality small molecule drug leads with enhanced therapeutic potential.
Pyramid™ defines a process by which a range of high-throughput biophysical and computational techniques are used to experimentally characterise the interactions of very low molecular weight compounds (fragments) with their target proteins. These fragments can then be rapidly and efficiently optimised into potent lead compounds using iterative medicinal chemistry guided and informed by structure-based design.
By careful monitoring of key characteristics such as ligand efficiency and in vivo activity during lead optimisation, 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 drug 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.