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.