Key words: kidney transplantation, immunosuppression, pharmacokinetics, tacrolimus, therapeutic drug monitoring

"Novel Insights for Improvement of Tacrolimus Therapy"

Individualization of tacrolimus treatment to prevent rejection in kidney transplantation is pivotal. It has been shown that:

• Tacrolimus can also be administered by a suppository, contrary to application under the tongue.
• Altered tacrolimus blood levels after steroid dose changes can partly be explained by genetic mechanisms.
• The newer once-daily formulation has a lower variability of drug exposure compared to the older twice-daily formulation, which is relevant since a higher variability is associated with worse graft survival.
• Similar to twice-daily tacrolimus, drug exposure of once-daily tacrolimus is acceptably lower when administered together with breakfast. Non-fasted intake can be allowed for convenience reasons, provided drug levels are monitored.
• Tacrolimus levels in the elimination phase of the newer once-daily tacrolimus formulation better predict drug exposure than the currently applied pre-dose levels.