Cell Cultures in Drug Discovery An Industrial Perspective

Anna-Lena Ungell and Johan Karlsson Abbreviations 

Cystic fibrosis transmembrane conductance exporter family 

Efflux ratio (transport basolateral to apical divided by transport apical to basolateral) 

N-2-hydroxyethyl-piperazine-N -2-ethanesulfonic acid High-throughput screening 

Liquid chromatography combined with mass spectrometry detection 

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Cell Cultures in Drug Discovery An Industrial Perspective... 

Ungell, A.-L. and Karlsson, J. (2003) Cell cultures in drug discovery an industrial perspective, in Drug Bioavailahility — Estimation of Solubility, Permeability and Absorption (eds H. van de Waterbeemd, H. Lennernas and P. Artursson), Wiley,... 

Ungell AL and Karlsson J. Cell Cultures in Drug Discovery An Industrial Perspective. In Van de Waterbeemd et al. eds.),Drug Bioavailability. Estimation of Solubility, Permeability, Absorption and Bioavailability. P. Wiley WCH 2003, pp. 72-89. 

Figure 9.11 Oral fraction absorbed in humans versus Caco-2 Papp for series of 25 compounds. (Reproduced with permission from Ungell, A.-L., Karlsson, J. Cell Cultures in Drug Discovery An Industrial Perspective , Chapter 5 in van de Waterbeemd, H., Lennernas, H., Artursson, P., Eds. Drug Bioavailahility 2003, (Wiley-VCH Verlag GmbH Co. KGaA) p. 107, copyright 2003).

From an industrial perspective, quantitative knowledge of the existence of different transporters within the cellular system used in screening procedures is of major importance as it can influence both the predictive value of the permeability coefficients and interpretation of the results. In addition, information on species differences or similarities or discrepancies between cell culture models and animals now provide an important basis for the scaling of data during the early phases of drug discovery for animals or humans [48]. 

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