It is worth mentioning that due to the strong hepatotoxicity of hydrophobic bile acids, the research and development of drugs that directly target the activation of hepatocyte detoxification enzymes (CYP3A4, UGT1A1, and SULT2A1) to accelerate the metabolism of hydrophobic bile acids to hydrophilic bile acids is also a very promising strategy for the development of drugs for the treatment of cholestasis. This evidence concerns the gene CYP3A4 and cholestasis.