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Updated: Dec 18, 2025

Quantification of the Immunosuppressant Tacrolimus on Dried Blood Spots Using LC-MS/MS
Published on: November 8, 2015
Thirty Years of Tacrolimus in Clinical Practice
Song C Ong1, Robert S Gaston1,2
1Department of Medicine, Division of Nephrology, University of Alabama at Birmingham, Birmingham, AL.
Tacrolimus, a key immunosuppressant, has been vital for organ transplantation since the 1980s. Despite toxicity concerns, its efficacy in preventing graft rejection remains crucial, with new combinations showing promise.
Area of Science:
- Immunology
- Pharmacology
- Transplantation Medicine
Background:
- Tacrolimus, discovered in 1984, revolutionized solid organ transplantation.
- Calcineurin-inhibitor toxicity has prompted research into minimizing its use, with limited success.
- Current focus emphasizes tacrolimus's efficacy in preventing graft rejection and loss.
Purpose of the Study:
- To review the development and evolving clinical utility of tacrolimus.
- To discuss current issues affecting tacrolimus usage in transplantation.
- To explore newer therapeutic combinations involving tacrolimus.
Main Methods:
- Literature review of tacrolimus development and clinical application.
- Analysis of studies on calcineurin-inhibitor toxicity and management.
- Examination of recent research on novel immunosuppressive combinations.
Main Results:
- Tacrolimus remains a cornerstone of immunosuppression in solid organ transplantation.
- Efforts to reduce calcineurin-inhibitor toxicity have yielded limited success.
- Novel combinations with everolimus and belatacept show potential for improved outcomes.
Conclusions:
- Tacrolimus continues to be essential for preventing graft rejection and loss.
- Ongoing research explores strategies to mitigate toxicity while preserving efficacy.
- Future directions include optimizing tacrolimus-based regimens with newer agents for enhanced patient benefits.
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