Title | Chirality and new drug development in 1995 | |
Authors | Charalampos T. Plessas1, Stavros T. Plessas2 and Achilles Benakis3
1. PHARMAKON-Press, Department of Scientific Informations, Athens, Greece 2. Laboratory of Physiology, Department of Nursing, University of Athens, Athens, Greece 3. Laboratory of Drug Metabolism, Department of Pharmacology, School of Medicine, University of Geneva, Geneva, Switzerland |
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Citation | Plessas, C.T., Plessas, S.T., Benakis, A.: Chirality and new drug development in 1995, Epitheorese Klin. Farmakol. Farmakokinet. 9(1): 3-20 (1995) | |
Publication Date | 1995 | |
Full Text Language | English | |
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Keywords | Chirality, stereoisomers, pharmacology, pharmacokinetics, drug development, enantiomeric separation, chromatography on chiral stationary phases, chromatography on chiral mobile phases, capillary zone electrophoresis, preparation, cost-benefit analysis, regulatory requirements. | |
Other Terms | review article | |
Summary | All living organisms are constituted by ordered asymmetric biomolecules, such as proteins (receptors, enzymes, antibodies), carbohydrates, neurotransmitters, hormones etc., due to the special geometry of one or more of their carbon atoms. The asymmetry is not only restricted to the biogenic compounds; a great number of xenobiotics, including drugs, thought to be monosubstances, are in fact racemic mixtures of two or more diastereoisomers. These stereoisomers (including enantiomers) may interact in different ways with biological structures and, therefore, may exhibit widely different pharmacodynamics and pharmacokinetic properties. These considerations justify the current trends, in pharmaceutical industry as well as in regulatory authorities, to develop the eutomer, i.e. the single enantiomer characterised by the most favourable pharmacological profile. The possibility to produce the eutomer is facilitated by the availability of new technologies for the stereoselective synthesis and separation of individual enantiomers from the racemic mixtures; these technologies include chiral stationary phases, chiral mobile phases and capillary zone electrophoresis. However, any decision to develop the eutomer should be based on careful consideration of production and development costs and actual therapeutic advantages especially in terms of improved safety. | |
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