Tacrolimus

(Prograf®)

Tacrolimus

Drug updated on 11/1/2024

Dosage FormCapsule (oral; 0.5 mg, 1 mg, 5 mg) Injection (intravenous; 5mg/mL) Granule (oral; 0.2 mg [1 mg])
Drug ClassCalcineurin inhibitor immunosuppressants
Ongoing and
Completed Studies
ClinicalTrials.gov

Indication

  • Indicated for the prophylaxis of organ rejection in adult and pediatric patients receiving allogeneic liver, kidney, heart, or lung transplants, in combination with other immunosuppressants.

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Summary
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  • This summary is based on the review of 16 systematic review(s)/meta-analysis(es). [1-16]
  • Combining genotype-informed and pharmacokinetic model-based dosing for tacrolimus in pediatric solid organ transplant (SOT) recipients shows potential for dosing accuracy, though evidence on the optimization of initial and subsequent doses remains limited.
  • GLP-1 receptor agonists (GLP-1RAs) significantly reduced urine protein ratio and hemoglobin A1c levels in kidney transplant recipients (KTRs) without impacting tacrolimus levels, suggesting possible benefits for metabolic and glycemic control in this population. 4. mTOR inhibitors were effective in a reduced tacrolimus regimen but increased rejection rates when calcineurin inhibitors were avoided or steroids withdrawn early. Once-daily tacrolimus was comparable to twice-daily formulations in acute rejection and renal function outcomes for de novo renal transplant patients.
  • The presence of the CYP3A4*22 allele was associated with higher plasma dose-adjusted trough concentrations (C(0)/D) of tacrolimus, indicating that lower doses may achieve therapeutic levels, supporting dose individualization based on genetic polymorphisms.
  • Tacrolimus is associated with nephrotoxicity, new-onset diabetes after transplantation (NODAT), and gastrointestinal toxicity; pharmacokinetic variability within and between individuals complicates management despite therapeutic drug monitoring.
  • GLP-1 receptor agonists (GLP-1RAs) in kidney transplant recipients had side effects including nausea and vomiting (17.6%), diarrhea (7.6%), and injection site pain (5.4%).
  • Belatacept increased risks of acute rejection and certain infections compared to tacrolimus, while mTOR inhibitors combined with reduced-dose tacrolimus showed increased rejection rates without higher rates of graft failure or death.

Product Monograph / Prescribing Information

Document TitleYearSource
Prograf (tacrolimus) Prescribing Information.2023Astellas Pharma US, Inc., Northbrook, IL

Systematic Reviews / Meta-Analyses

Document TitleYearSource
Evaluating the evidence for genotype-informed Bayesian dosing of tacrolimus in children undergoing solid organ transplantation: A systematic literature review2024British Journal of Clinical Pharmacology
Safety and efficacy of glucagon-like peptide-1 receptor agonists among kidney transplant recipients: a systematic review and meta-analysis2024Clinical Kidney Journal
A Comprehensive Mixed-Method Approach to Characterize the Source of Diurnal Tacrolimus Exposure Variability in Children: Systematic Review, Meta-analysis, and Application to an Existing Data Set2024Journal of Clinical Pharmacology
Comparative Safety and Efficacy of Immunosuppressive Regimens Post-kidney Transplant: A Systematic Review2023Cureus
Use of everolimus following kidney transplantation during pregnancy: A case report and systematic review2023Taiwanese Journal of Obstetrics & Gynecology
Individualized dosing algorithms for tacrolimus in kidney transplant recipients: current status and unmet needs2023Expert Opinion On Drug Metabolism & Toxicology
Effects of CYP3A4*22 polymorphism on trough concentration of tacrolimus in kidney transplantation: a systematic review and meta-analysis2023Frontiers in Pharmacology
Efficacy and safety of once-daily prolonged-release tacrolimus versus twice-daily tacrolimus in kidney transplant recipients: A meta-analysis and trial sequential analysis2023Journal of the Chinese Medical Association
Mammalian Target of Rapamycin Inhibitors and Kidney Function After Thoracic Transplantation: A Systematic Review and Recommendations for Management of Lung Transplant Recipients2023Transplantation
Belatacept in Kidney Transplantation: What Are the True Benefits? A Systematic Review2022Frontiers in Medicine
Efficacy and Safety of Tacrolimus-Based Maintenance Regimens in De Novo Kidney Transplant Recipients: A Systematic Review and Network Meta-Analysis of Randomized Controlled Trials2021Annals of Transplantation
Outcomes of Interleukin-2 Receptor Antagonist Induction Therapy in Standard-Risk Renal Transplant Recipients Maintained on Tacrolimus: A Systematic Review and Meta-Analysis2021American Journal of Nephrology
Identifying the association between tacrolimus exposure and toxicity in heart and lung transplant recipients: A systematic review2021Transplantation Reviews
Systematic external evaluation of published population pharmacokinetic models for tacrolimus in adult liver transplant recipients2020European Journal of Pharmaceutical Sciences
Once-Daily versus Twice-Daily Tacrolimus in Kidney Transplantation: A Systematic Review and Meta-analysis of Observational Studies2019Drugs
Toward a robust tool for pharmacokinetic-based personalization of treatment with tacrolimus in solid organ transplantation: A model-based meta-analysis approach2019British Journal of Clinical Pharmacology

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