Tacrolimus

(Prograf®)

Tacrolimus

Drug updated on 7/25/2024

Dosage FormCapsule (oral; 0.5 mg, 1 mg, 5 mg) Injection (intravenous; 5mg/mL) Granule (oral; 0.2 mg [1 mg])
Drug ClassCalcineurin-inhibitor immunosuppressant
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.

Latest News

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Summary
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  • Tacrolimus (Prograf) is 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.
  • The information was derived from 14 systematic reviews/meta-analyses studies focusing on tacrolimus' safety and effectiveness compared to other immunosuppressants.
  • Neurologic adverse effects such as tremor, headache, and insomnia were inconsistently correlated with tacrolimus trough concentrations; older age and female gender (especially Black females) showed higher incidences of these side effects.
  • Pharmacokinetic variability limits therapeutic drug monitoring's ability to prevent toxicity effectively; developed algorithms improved target concentration ranges but did not significantly reduce toxicity compared to bodyweight-based dosing.
  • No significant differences were found between once-daily versus twice-daily tacrolimus regimens regarding clinical outcomes like acute rejection rates or patient mortality in renal transplant patients.
  • Combining mTOR inhibitors with reduced tacrolimus exposure appears safer than calcineurin inhibitor avoidance or early steroid withdrawal regimens which show increased rejection rates.
  • Genetic polymorphisms such as CYP3A4*22 influence plasma concentrations and dose requirements for tacrolimus; personalized dosing based on genetic markers may improve safety and efficacy profiles over standard practices.

Product Monograph / Prescribing Information

Document TitleYearSource
Prograf (tacrolimus) prescribing information.2023Astellas Pharma US, Inc., Northbrook, IL

Systematic Reviews / Meta-Analyses

Document TitleYearSource
The association between tacrolimus exposure and tremor, headache and insomnia in adult kidney transplant recipients: a systematic review.2024Transplantation Reviews
Individualized dosing algorithms for tacrolimus in kidney transplant recipients: Current status and unmet needs.2023Expert Opinion on Drug Metabolism & Toxicology
Efficacy and safety of once-daily prolonged-release tacrolimus versus twice-daily tacrolimus in kidney transplant recipients: a meta-analysis and trial sequential analysis.2023Journal of the Chinese Medical Association
Comparative safety and efficacy of immunosuppressive regimens post-kidney transplant: a systematic review.2023Cureus
Effects of CYP3A4*22 polymorphism on trough concentration of tacrolimus in kidney transplantation: a systematic review and meta-analysis. 2023Frontiers in Pharmacology
Use of everolimus following kidney transplantation during pregnancy: a case report and systematic review.2023Taiwanese Journal of Obstetrics & Gynecology
Belatacept in kidney transplantation: What are the true benefits? A systematic review.2022Frontiers 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 trials.2021Annals of Transplantation
Safety and effectiveness of mycophenolate mofetil associated with tacrolimus for liver transplantation immunosuppression: a systematic review and meta-analysis of randomized controlled trials.2021Clinics
Population pharmacokinetic models of tacrolimus in adult transplant recipients: a systematic review.2020Clinical Pharmacokinetics
Use of T Cell mediated immune functional assays for adjustment of immunosuppressive or anti-infective agents in solid organ transplant recipients: a systematic review.2020Frontiers in Immunology
Regulatory cell therapy in kidney transplantation (The ONE Study): a harmonised design and analysis of seven non-randomised, single-arm, phase 1/2A trials.2020Lancet
Comparison of tacrolimus and cyclosporine combined with methotrexate for graft versus host disease prophylaxis after allogeneic hematopoietic cell transplantation.2020Transplantation
Once-daily versus twice-daily tacrolimus in kidney transplantation: a systematic review and meta-analysis of observational studies.2019Drugs

Clinical Practice Guidelines