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Quantification of the Immunosuppressant Tacrolimus on Dried Blood Spots Using LC-MS/MS
08:38

Quantification of the Immunosuppressant Tacrolimus on Dried Blood Spots Using LC-MS/MS

Published on: November 8, 2015

Modified release tacrolimus

M Roy First1, William E Fitzsimmons

  • 1Research and Development, Fujisawa Healthcare, Inc., Three Parkway North, Deerfield, IL 60015-2548, USA. roy_first@fujisawa.com

Yonsei Medical Journal
|January 1, 2005
PubMed

Insights

Modified Release tacrolimus offers similar exposure to Prograf but with reduced peak levels. Stable kidney and liver transplant patients can safely switch to once-daily MR tacrolimus, potentially improving compliance.

Area of Science:

  • Pharmacology
  • Transplantation Medicine
  • Drug Formulation

Background:

  • Tacrolimus (Prograf) is a key immunosuppressant post-transplant.
  • Standard tacrolimus dosing is twice daily (bid).
  • Modified Release (MR) tacrolimus offers once-daily (qd) dosing.

Purpose of the Study:

  • To evaluate pharmacokinetics of MR tacrolimus in transplant recipients.
  • To assess safety and efficacy of converting from Prograf bid to MR tacrolimus qd.
  • To compare exposure and variability between tacrolimus formulations.

Main Methods:

  • Pharmacokinetic studies in stable kidney and liver transplant recipients.
  • Conversion from Prograf bid to MR tacrolimus qd (mg-for-mg daily dose).
  • Analysis of exposure (AUC), trough levels (Cmin), and peak levels (Cmax).

Main Results:

  • MR tacrolimus qd demonstrated similar exposure (AUC) and trough levels (Cmin) to Prograf bid in healthy volunteers.
  • Steady-state exposure and target trough levels were equivalent after conversion in transplant patients.
  • Significantly less intra-subject variability in exposure was observed with MR tacrolimus.

Conclusions:

  • Stable kidney and liver transplant recipients can be safely converted to MR tacrolimus qd.
  • A mg-for-mg daily dose conversion is effective.
  • Once-daily MR tacrolimus may improve patient compliance while maintaining immunosuppression.

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