Drug updated on 5/17/2024

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


  • 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

loading GIF

This AI-generated content is provided without warranty, with no liability accepted for reliance on it. Learn more.

  • Tacrolimus (Prograf) is indicated for the prophylaxis of organ rejection in adult and pediatric patients receiving allogeneic liver, kidney, heart, or lung transplants. It is used in combination with other immunosuppressants.
  • Fourteen studies were reviewed to gather information about Tacrolimus. These studies focused on its safety and effectiveness as an immunosuppressant in organ transplant recipients.
  • Neurological side effects such as tremor, headache, and insomnia are not significantly associated with tacrolimus trough concentrations, but toxicity requiring dose reduction is more common at supratherapeutic levels. Females, particularly Black females, along with elderly individuals, are more susceptible to these neurological side effects, indicating a need for careful dose adjustment.
  • Nephrotoxicity and post-transplant diabetes mellitus have been linked to tacrolimus use, despite therapeutic drug monitoring aimed at minimizing toxicity due to highly variable pharmacokinetics of the drug.
  • When compared with mTOR inhibitors, which can reduce exposure without compromising safety or efficacy; genetic polymorphisms like CYP3A4*22 also influence dosing requirements, suggesting that personalized medicine approaches may be beneficial.
  • In terms of regimen comparison: Combining Tacrolimus (Prograf) with mycophenolate mofetil shows superior effectiveness in preventing acute rejection than using Prograf alone, without increasing adverse events, making it safe for liver transplantation procedures.
  • Pregnancy considerations show no teratogenicity identified from babies exposed to everolimus, often used alongside Prograf, implying potential safety during the pregnancy period.
  • The once-daily formulation has similar rates of graft failure, death, and adverse events within the first year after renal transplant compared to the twice-daily version, thus improving adherence without compromising outcomes. Long-term studies suggest comparable rates between both formulations regarding acute rejection, graft loss, patient mortality, hence showing broadly similar efficacy profiles.

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