Role of P-glycoprotein and cytochrome P450 3A in limiting oral absorption of peptides and peptidomimetics.

@article{Wacher1998RoleOP,
  title={Role of P-glycoprotein and cytochrome P450 3A in limiting oral absorption of peptides and peptidomimetics.},
  author={Vincent J. Wacher and Jason A Silverman and Ying Zhang and Leslie Z Benet},
  journal={Journal of pharmaceutical sciences},
  year={1998},
  volume={87 11},
  pages={1322-30}
}
Cytochrome P450 3A4 (CYP3A4), the major phase I drug metabolizing enzyme in humans, and the MDR1 gene product P-glycoprotein (P-gp) are present at high concentrations in villus tip enterocytes of the small intestine and share a significant overlap in substrate specificity. A large body of research both in vitro and in vivo has established metabolism by intestinal CYP3A4 as a major determinant of the systemic bioavailability of orally administered drugs. More recently it has been recognized that… CONTINUE READING
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