Molecular mechanisms on drug transporters in the drug absorption and disposition

Satohiro Masuda, Ken Inui

Research output: Contribution to journalReview articlepeer-review

1 Citation (Scopus)


The membrane transport processes of drugs are critical issues to determine their absorption, distribution and elimination. Recently, various drug transporters have been identified and characterized. The enterocyte peptide transporter PEPT1 mediates the absorption of peptide-like drugs including beta-lactam antibiotics as well as valacyclovir lacking peptide bond. In the kidney, the basolateral organic anion transporters (OAT1, OAT3) and cation transporters (OCT1, OCT2) mediate renal distribution of hydrophilic anionic and cationic drugs, respectively. The brush-border type OAT-K1/K2 were suggested to be a target transporter for methotrexate-leucovorine rescue therapy. The ATP-driven efflux pump P-glycoprotein appeared to be an interaction site between digoxin and clarithromycin or itraconazole in the kidney. In addition, the intestinal P-glycoprotein was suggested to act as an absorptive barrier for tacrolimus in recipients of liver and small bowel transplantation.

Original languageEnglish
Pages (from-to)65-73
Number of pages9
JournalNippon rinsho. Japanese journal of clinical medicine
Issue number1
Publication statusPublished - Jan 2002
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • General Medicine


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