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Sartorius

Reveal the Secrets and Expand the Boundaries of Early Drug Discovery

Reveal the Secrets and Expand the Boundaries of Early Drug Discovery


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Sartorius

For small-molecule drugs and biologics alike, the path to a marketed drug involves a long and exhaustive journey through basic research, discovery of the medicine, preclinical development tests, increasingly complicated clinical trials, and finally the regulatory approval. While traditional biochemical analysis methods such as ELISA and western blots are still used, more and more scientists are adapting label-free analytical techniques in their workflows.

These techniques include systems that convert biomolecular interactions into response signals, often in real-time, providing researchers with additional capabilities to characterizing binding mechanisms. These systems can be used for kinetics characterization, concentration determination and biomolecular interactions screening amongst other things. Label-free technologies provide on- and off-rates (ka and kd) in kinetic characterization experiments which are key determinants in affinity constant (KD) derivation and information not available with end-point analysis techniques such as ELISA.

Some commonly used label-free technologies include isothermal titration calorimetry (ITC), surface plasmon resonance (SPR) and Bio-Layer Interferometry (BLI). Each technique has its own unique advantages. With so many options to choose from, researchers going for techniques that move drug candidates rapidly and accurately through the various stages of the drug development process. Of these common label-free techniques, ITC is versatile at providing rich thermodynamics data, but does not provide kinetics-rich information, such as ka and kd values, during an interaction study. SPR and BLI, while not as rich in thermodynamics data extraction, both provide affinity characterization data with additional information, such as ka and kd values.

The Octet® BLI platform offers distinct benefits that sets it apart as a desirable technology for accelerating early drug discovery. The Octet® BLI platform utilizes 96- or 384-well sample plates, with the instrument’s read head moving the sensor tips directly into the sample plate. This fluidic-free approach is distinctly different allowing greater tolerance for the most challenging samples.

The instruments are easy to use, and therefore require relatively less analyst skill to operate compared to SPR instruments, and do not require sample loading times or cleaning between samples. These attributes, combined with the capability to simultaneously analyze up to 96 samples at a time, makes them an ideal lead selection system for early drug discovery and an indispensable tool for the development process, process optimization as well as the final quality control (QC) of new biotherapeutics under GxP.