Predicting the extent of metabolism using in vitro permeability rate measurements and in silico permeability rate predictions.

ABSTRACT: The Biopharmaceutics Drug Disposition Classification System (BDDCS) can be utilized to predict drug disposition, including interactions with other drugs and transporter or metabolizing enzyme effects based on the extent of metabolism and solubility of a drug. However, defining the extent of metabolism relies upon clinical data. Drugs exhibiting high passive intestinal permeability rates are extensively metabolized. Therefore, we aimed to determine if in vitro measures of permeability rate or in silico permeability rate predictions could predict the extent of metabolism, to determine a reference compound representing the permeability rate above which compounds would be expected to be extensively metabolized, and to predict the major route of elimination of compounds in a two-tier approach u

SUBMITTER: Hosey CM 

PROVIDER: S-EPMC4666302 | biostudies-literature | 2015 May

REPOSITORIES: biostudies-literature