Abstract
The observation that chirality can play a major role in the toxicity and specificity of therapeutic agents was first made in 1956 by Carl Pfeiffer1 and is commonly referred to as Pfeiffer’s Rule: “…the greater the difference between the pharmacological activity of the D and L isomers, the greater is the specificity of the active isomer for the response of the tissue under test.” Indeed, the vast majority of medicines are chiral, and worldwide sales of chiral drugs in single-enantiomer dosage forms represented a market of $133 billion in 2000.2 Currently, 40% of all dosage-form drug sales are of single enantiomers, up from 30% in 1999, and this proportion will grow in accordance with FDA policy since the wrong enantiomer can cause harmful side effects.
© 2002 Optical Society of America
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