Abstract The sections in this article are: Foreign Substance Metabolism by the Intestinal Mucosa Nonsynthetic Reactions Synthetic Reactions Multiplicity of Biotransformation Reactions Species and Strain Differences Fetal Development and Phylogenetic Aspects Biotransformation by Intestinal Microorganisms Adaptation of Xenobiotic Metabolism in the Gastrointestinal Tract Endogenous Compounds in Regulation of Drug Metabolism Enhancement of Biotransformation by Exogenous Compounds Effect of Luminal Contents Interaction of Intestinal Microflora and Mucosal Functions Concluding Remarks