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BIOCHEMISTRY AND METABOLISM |
 | BIOCHEMISTRY AND METABOLISM
New drug discovery approach requires an early evaluation of toxicological and ADME characteristics of new chemical entities, together with the in vitro investigation of drug metabolism, drug-drug-interactions and transepithelium permeability.
IN VITRO CYTOTOXICITY
The potential cytotoxicity of test compounds can be assessed by incubation with human or animal hepatocytes or cultures of special cell lines. | | | DRUG METABOLISM-INTERSPECIES COMPARISON
In vitro metabolism of test compounds is assessed by monitoring the disappearance of the parent compound and/or the appearance of metabolites. The interspecies comparison of metabolic profile (using rat, dog, monkey and human microsomes) can help to choose the second species in tox studies.
TRANSEPITHELIUM PERMEABILITY
The compound permeability, expressed as apparent permeability coefficient, is evaluated in the apical to basolateral and basolateral to apical directions. Transport mechanisms are evaluated in relation to P-glycoprotein (Pgp) role, using specific Pgp inhibitors. |  |
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BIOCHEMISTRY AND METABOLISM