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Enantiomerism or drug chirality is one of the major concerns in drug discovery and development since more than 50% of currently marketed drugs are chiral compounds. Chiral molecules are also called enantiomers where a molecule contains at least one asymmetric carbon. Chiral inversion is an important phenomenon in which an enantiomer may convert from one enantiomeric configuration to the other which can be unidirectional or bidirectional. Enantiomers, though similar in their chemical structure, show noticeable differences in their biological properties. Therefore, a thorough knowledge of racemic drugs is important in the drug developmental stages to eliminate inactive or toxic isomers. Different databases such as ‘ScienceDirect’ and ‘Google Scholar have been used to search the articles using keywords Absorption of chiral compounds; Chirality in pharmacology; Enantiomers; Enantioselectivity; and Pharmacokinetics. With the advancement in synthetic chemistry, the development of a single enantiomer could potentially improve the overall development and manufacturing process of drugs. The current review addresses the nomenclature and enantioselectivity of enantiomers in various pharmacokinetic parameters such as absorption, distribution, metabolism and excretion.
Enantiomerism or drug chirality is one of the major concerns in drug discovery and development since more than 50% of currently marketed drugs are chiral compounds. Chiral molecules are also called enantiomers where a molecule contains at least one asymmetric carbon. Chiral inversion is an important phenomenon in which an enantiomer may convert from one enantiomeric configuration to the other which can be unidirectional or bidirectional. Enantiomers, though similar in their chemical structure, show noticeable differences in their biological properties. Therefore, a thorough knowledge of racemic drugs is important in the drug developmental stages to eliminate inactive or toxic isomers. Different databases such as ‘ScienceDirect’ and ‘Google Scholar have been used to search the articles using keywords Absorption of chiral compounds; Chirality in pharmacology; Enantiomers; Enantioselectivity; and Pharmacokinetics. With the advancement in synthetic chemistry, the development of a single enantiomer could potentially improve the overall development and manufacturing process of drugs. The current review addresses the nomenclature and enantioselectivity of enantiomers in various pharmacokinetic parameters such as absorption, distribution, metabolism and excretion.
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