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Joint DIA/MHRA Statistics Workshop 2nd-4th October 2013, London, United Kingdom
| By Drug Information Association
Life-cycle management is a widely accepted concept for the development and marketing of medicines. At each step of this process, pre- and post-licensing, statisticians work to develop methods that can improve efficiency and can enhance decision-making through optimal study design, analysis and inference. The workshop aims to discuss the latest developments in statistical methodology and decision-making in exploratory development, confirmatory development, licensing decisions and management of benefits and risks post-licensing.
Regulatory Affairs > White Papers
Journal of Biomolecular Screening
| By ZoBio
Fragment-based drug discovery (FBDD) has become a widely accepted tool that is complementary to high-throughput screening (HTS) in developing small-molecule inhibitors of pharmaceutical targets. Because a fragment campaign can only be as successful as the hit matter found, it is critical that the first stage of the process be optimized. Here the authors compare the 3 most commonly used methods for hit discovery in FBDD: high concentration screening (HCS), solution ligandobserved nuclear magnetic resonance (NMR), and surface plasmon resonance (SPR). They selected the commonly used saturation transfer difference (STD) NMR spectroscopy and the proprietary target immobilized NMR screening (TINS) as representative of the array of possible NMR methods. Using a target typical of FBDD campaigns, the authors find that HCS and TINS are the most sensitive to weak interactions. They also find a good correlation between TINS and STD for tighter binding ligands, but the ability of STD to detect ligands with affinity weaker than 1 mM KD is limited. Similarly, they find that SPR detection is most suited to ligands that bind with KD better than 1 mM. However, the good correlation between SPR and potency in a bioassay makes this a good method for hit validation and characterization studies.
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