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J Basic Clin Pharm. 2010 Mar;1(2):63-9. Epub 2010 May 15.

Caco-2 cell lines in drug discovery- an updated perspective.

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Department of Pharmacy, School of Chemical & Biotechnology, SASTRA University, Thanjavur-613401, Tamilnadu, India.


Cell lines are the invitro models used for the drug permeability studies in the preclinical and clinical phases of the drug discovery. Cell line models are simple and quick to use and avoids the usage of animal models for pharmacological and toxicological studies and hence cost effective, produce reliable and reproducible results for understanding and evaluating the permeability characteristics of the potential lead drug candidates. Different cell line models used in the drug permeability studies, their characteristics has been summarized emphasizing on CACO-2. By virtue of its merits, CACO-2 cell line development, transport experiments, automated assays, optimization of experimental conditions and mechanistic uses of CACO-2 cell lines dealt comprehensively in the following context.


CACO-2; Drug candidates; Drug discovery; Drug premeability; invitro cell lines


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