Chiral Drugs: An Overview

By Lien Ai Nguyen, Hua He, C. Pham-Huy. International Journal of Biomedical Science, 2006

647 citations recorded by the source corpus.

About more than half of the drugs currently in use are chiral compounds and near 90% of the last ones are marketed as racemates consisting of an equimolar mixture of two enantiomers. Although they have the same chemical structure, most isomers of chiral drugs exhibit marked differences in biological activities such as pharmacology, toxicology, pharmacokinetics, metabolism etc. Some mechanisms of these properties are also explained. Therefore, it is important to promote the chiral separation and analysis of racemic drugs in pharmaceutical industry as well as in clinic in order to eliminate the unwanted isomer from the preparation and to find an optimal treatment and a right therapeutic control for the patient. In this article, we review the nomenclature, pharmacology, toxicology, pharmacokinetics, metabolism etc of some usual chiral drugs as well as their mechanisms. Different techniques used for the chiral separation in pharmaceutical industry as well as in clinical analyses are also examined.

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Citations in the corpus

Geometric deep learning on molecular representations (2021, background): “Chirality plays a key role in chemical biology; relevant examples of chiral molecules are DNA, and several drugs whose enantiomers exhibit markedly different pharmacological and toxicological properties [64].”
Free Radicals, Antioxidants in Disease and Health (2008, background): “Even if antioxidant supplementation is receiving enthusiastic debate and is increasingly adopted in many industrial countries, supporting evidence is still ambiguous (5-59).”
Polarization control in an X-ray free-electron laser (2016, background): “Research in these areas includes novel designs for spin control toward all-optical data storage [3], the control of chiral pharmaceuticals [4], and efforts to understand the origin of the homochirality of life [5].”