Lead Optimization

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Lead optimization is the synthetic modification of a biologically active compound, to fulfill all stereoelectronic, physicochemical, pharmacokinetic and toxicologic requirements for clinical usefulness.It is a process to optimize the molecules or compounds that demonstrate the potential to be transformed into drugs, retaining only a small number of them for the next stages.

The Lead Optimization process compares the properties of various lead compounds and provides information to help select the leads with the greatest potential to be developed into safe and effective medicines, and in alignment with corporate strategy. Often during this stage of development, lead prioritization studies are conducted in living organisms (in vivo) and in cells in the test tube (in vitro) to compare various lead compounds and how they are metabolized and affect the body.