Send to

Choose Destination
See comment in PubMed Commons below
Ther Drug Monit. 2006 Feb;28(1):39-44.

Active drug transport of immunosuppressants: new insights for pharmacokinetics and pharmacodynamics.

Author information

  • 1Clinical Research and Development, Department of Anesthesiology, University of Colorado Health Sciences Center, Denver, Colorado 80262, USA.


Immunosuppressants have a narrow therapeutic index, and pharmacokinetic variability negatively affects long-term outcome of transplantation. Recently, it has become clear that active transport is a major determinant of the inter-and intraindividual variability of the pharmacokinetics and pharmacodynamics of immunosuppressants. Active transport plays a key role in (1) the poor correlation between oral doses and systemic exposure of cyclosporine, tacrolimus, sirolimus, and everolimus, (2) tissue distribution including distribution into lymphocytes, (3) hepatic and intestinal metabolism, (4) the pharmacokinetic variability of immunosuppressants after oral dosing, (5) drug-drug interactions, (6) disease-drug interactions, and (7) age, gender, and ethnicity-based differences in pharmacokinetics of immunosuppressants. Those new insights may significantly improve patient management and long-term outcome not only by reducing pharmacokinetic variability and avoidance of drug-drug interactions but also by identification of sensitive patient populations. They will also significantly impact preclinical and clinical development strategies of new immunosuppressants.

[PubMed - indexed for MEDLINE]
PubMed Commons home

PubMed Commons

How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for Lippincott Williams & Wilkins
    Loading ...
    Write to the Help Desk