Development and regulation of chiral drug substances: an overview on worldwide pharmaceutical guidelines

ABSTRACT

Optical rotation, the ability of a substance to rotate the plane of the polarized light, was known since 1815. The proposal of Louis Pasteur in 1848 made it clear that the optical activity of organic solution is determined by molecular asymmetry, wich produces non-superimposable mirror-image structures (Drayer, 1993). Since discovery and exploitation of chiral pharmaceuticals for clinical use, major advances have been made regarding stereoselective pharmacological activity, differential pharmacokinetics, pharmacodynamics profiles, their toxicological divergences and recently economical interests. These factors made it necessary the drug authorities of several countries to publish and adopt guidelines...