Tacrolimus

Tacrolimus binds to an intracellular protein, FKBP-12. A complex of tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin (a ubiquitous mammalian intracellular enzyme) is then formed, after which the phosphatase activity of calcineurin is inhibited.

• Tacrolimus capsules are calcineurin-inhibitor immunosuppressant indicated for the prophylaxis of organ rejection in adult patients receiving allogeneic liver, kidney or heart transplants and pediatric patients receiving allogeneic liver transplants in combination with other immunosuppressants. ( 1.1 ) 1.1 Prophylaxis of Organ Rejection in Kidney, Liver or Heart Transplant Tacrolimus capsules are indicated for the prophylaxis of organ rejection, in adult patients receiving allogeneic kidney transplant [ see Clinical Studies (14.1) ] , liver transplants [ see Clinical Studies (14.2) ] and heart transplant [ see Clinical Studies (14.3) ] , and pediatric patients receiving allogeneic liver transplants [ see Clinical Studies (14.2) ] in combination with other immunosuppressants.

• Tacrolimus capsules are contraindicated in patients with a hypersensitivity to tacrolimus. Tacrolimus injection is contraindicated in patients with a hypersensitivity to HCO-60 (polyoxyl 60 hydrogenated castor oil).contraindicated

• Intravenous (IV) use recommended for patients who cannot tolerate oral formulations (capsules). ( 2.1 , 2.2 ) • Administer capsules consistently with or without food. ( 2.1 ) • Therapeutic drug monitoring is recommended. ( 2.1 , 2.6 ) • Avoid eating grapefruit or drinking grapefruit juice. ( 2.1 ) • See dosing adjustments for African-American patients ( 2.2 ), hepatic and renal impaired. ( 2.4 , 2.5 ) • For complete dosing information, see the Full Prescribing Information . ADULT Patient Population Initial Oral Dosage (formulation) Whole Blood Trough Concentration Range Kidney Transplant With azathioprine 0.2 mg/kg/day capsules, divided in two doses, every 12 hours Month 1 to 3: 7 to 20 ng/mL Month 4 to 12: 5 to 15 ng/mL With MMF/IL-2 receptor antagonist 0.1 mg/kg/day capsules, divided in two doses, every 12 hours Month 1 to 12: 4 to 11 ng/mL Liver Transplant With corticosteroids only 0.1 to 0.15 mg/kg/day capsules, divided in two doses, every 12 hours Month 1 to 12: 5 to 20 ng/mL Heart Transplant With azathioprine or MMF MMF= Mycophenolate mofetil 0.075 mg/kg/day capsules, divided in two doses, every 12 hours Month 1 to 3: 10 to 20 ng/mL Month ≥ 4: 5 to 15 ng/mL PEDIATRIC Liver Transplant 0.15 to 0.2 mg/kg/day capsules divided in two doses, every 12 hours Month 1 to 12: 5 to 20 ng/mL 2.1 Important Administration Instructions Tacrolimus capsules should not be used without supervision by a physician with experience in immunosuppressive therapy. Tacrolimus capsules are not interchangeable or substitutable for other tacrolimus extended-release products.

Not Interchangeable with Extended Release Tacrolimus Products-Medication Errors : Instruct patients or caregivers to recognize the appearance of tacrolimus capsules. ( 5.3 ) New Onset Diabetes After Transplant: Monitor blood glucose. ( 5.4 ) Nephrotoxicity (acute and/or chronic): Reduce the dose; use caution with other nephrotoxic drugs. ( 5.5 ) Neurotoxicity: Including risk of Posterior Reversible Encephalopathy Syndrome (PRES), monitor for neurologic abnormalities; reduce or discontinue tacrolimus. ( 5.6 ) Hyperkalemia: Monitor serum potassium levels. Consider carefully before using with other agents also associated with hyperkalemia. ( 5.7 ) Hypertension: May require antihypertensive therapy. Monitor relevant drug-drug interactions. ( 5.8 ) Anaphylactic Reactions with IV formulation: Observe patients receiving tacrolimus injection for signs and symptoms of anaphylaxis. ( 5.9 ) Not recommended for use with sirolimus: Not recommended in liver and heart transplant due to increased risk of serious adverse reactions. ( 5.10 ) Myocardial Hypertrophy: Consider dose reduction/discontinuation. ( 5.13 ) Immunizations: Avoid live vaccines. ( 5.14 ) Pure Red Cell Aplasia: Consider discontinuation of tacrolimus. ( 5.15 ) Thrombotic Microangiopathy, Including Hemolytic Uremic Syndrome and Thrombotic Thrombocytopenic Purpura: May occur, especially in patients with infections and certain other concomitant medications.

The following serious and otherwise important adverse drug reactions are discussed in greater detail in other sections of labeling: • Lymphoma and Other Malignancies [ see Warnings and Precautions (5.1) ] • Serious Infections [ see Warnings and Precautions (5.2) ] • New Onset Diabetes After Transplant [ see Warnings and Precautions (5.4) ] • Nephrotoxicity [ see Warnings and Precautions (5.5) ] • Neurotoxicity [ see Warnings and Precautions (5.6) ] • Hyperkalemia [ see Warnings and Precautions (5.7) ] • Hypertension [ see Warnings and Precautions (5.8) ] • Anaphylactic Reactions with Tacrolimus Injection [ see Warnings and Precautions (5.9) ] • Myocardial Hypertrophy [ see Warnings and Precautions (5.13) ] • Pure Red Cell Aplasia [ see Warnings and Precautions (5.15) ] • Thrombotic Microangiopathy, Including Hemolytic Uremic Syndrome and Thrombotic Thrombocytopenic Purpura [ see Warnings and Precautions (5.16) ] The most common adverse reactions (≥ 15%) were abnormal renal function, hypertension, diabetes mellitus, fever, CMV infection, tremor, hyperglycemia, leukopenia, infection, anemia, bronchitis, pericardial effusion, urinary tract infection, constipation, diarrhea, headache, abdominal pain, insomnia, paresthesia, peripheral edema, nausea, hyperkalemia, hypomagnesemia, and hyperlipemia. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Biocon Pharma Inc., at 1-866-924-6266 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .

Pregnancy: Can cause fetal harm. Advise pregnant women of the potential risk to the fetus. ( 8.1 , 8.3 ) Additional pediatric use information is approved for Astellas Pharma US, Inc.’s Prograf (tacrolimus) products. However, due to Astellas Pharma US, Inc.’s marketing exclusivity rights, this drug product is not labeled with that information 8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy registry that monitors pregnancy outcomes in women exposed to tacrolimus during pregnancy. The Transplantation Pregnancy Registry International (TPRI) is a voluntary pregnancy exposure registry that monitors outcomes of pregnancy in female transplant recipients and those fathered by male transplant recipients exposed to immunosuppressants including tacrolimus. Healthcare providers are encouraged to advise their patients to register by contacting the Transplantation Pregnancy Registry International at 1-877-955-6877 or https://www.transplantpregnancyregistry.org/. Risk Summary Tacrolimus can cause fetal harm when administered to a pregnant woman. Data from postmarketing surveillance and TPRI suggest that infants exposed to tacrolimus in utero are at a risk of prematurity, birth defects/congenital anomalies, low birth weight, and fetal distress [see Human Data]. Advise pregnant women of the potential risk to the fetus.

Metabolism

Tacrolimus activity is primarily due to the parent drug. The pharmacokinetic parameters (mean ± S.D.) of tacrolimus have been determined following intravenous (IV) and/or oral (PO) administration in healthy volunteers, and in kidney transplant, liver transplant, and heart transplant patients (Table 17).

Limited overdosage experience is available. Acute overdosages of up to 30 times the intended dose have been reported. Almost all cases have been asymptomatic and all patients recovered with no sequelae. Acute overdosage was sometimes followed by adverse reactions consistent with those reported with the use of tacrolimus [see Adverse Reactions ( 6.1 ,6.2) ] , including tremors, abnormal renal function, hypertension, and peripheral edema; in one case of acute overdosage, transient urticaria and lethargy were observed. Based on the poor aqueous solubility and extensive erythrocyte and plasma protein binding, it is anticipated that tacrolimus is not dialyzable to any significant extent; there is no experience with charcoal hemoperfusion. The oral use of activated charcoal has been reported in treating acute overdoses, but experience has not been sufficient to warrant recommending its use. General supportive measures and treatment of specific symptoms should be followed in all cases of overdosage.

• Apr 8, 1994NDANDA050709Astellas
• Apr 8, 1994NDANDA050708Astellas
• Dec 8, 2000NDANDA050777Leo Pharma As
• Aug 10, 2009ANDAANDA065461Sandoz
• May 12, 2010ANDAANDA090509Dr Reddys Labs Ltd
• Jul 19, 2013NDANDA204096Astellas
• Jul 10, 2015NDANDA206406Veloxis Pharms Inc
• May 24, 2018NDANDA210115Astellas

1. 1Off Label Use14,6989.6%
2. 2Drug Ineffective10,0906.6%
3. 3Drug Interaction6,3374.2%
4. 4Product Use In Unapproved Indication6,2504.1%
5. 5Acute Kidney Injury5,9693.9%
6. 6Diarrhoea5,8573.8%
7. 7Death4,9953.3%
8. 8Transplant Rejection4,9843.3%
9. 9Pyrexia4,8143.2%
10. 10Cytomegalovirus Infection4,5613.0%
11. 11Pneumonia4,4722.9%
12. 12Covid-193,9272.6%
13. 13Toxicity To Various Agents3,8132.5%
14. 14Renal Impairment3,6272.4%
15. 15Sepsis3,4622.3%

Recent PubMed references pinned to Tacrolimus as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Tacrolimus as Single-Agent Immunotherapy for Adult-Onset Myasthenia Gravis: Remission, Relapse, and Safety.
  CNS neuroscience & therapeutics · 2026 · Geng Z, Jiang Y, Xie N, et al.
  PMID 42223343DOI 10.1002/cns.70921
• Timing matters: tacrolimus intra-patient variability within the initial seven months forecasts de novo DSA and subsequent rejection in a Chinese kidney transplant cohort.
  Frontiers in immunology · 2026 · Wang X, You J, Sun H, et al.
  PMID 42199410DOI 10.3389/fimmu.2026.1809202
• Localized Tacrolimus Delivery for Peripheral Nerve Regeneration: Molecular Mechanisms, Biomaterial Platforms, and Translational Strategies.
  International journal of molecular sciences · 2026 · Katturajan R, Shah SN, Crabtree J, et al.
  PMID 42196163DOI 10.3390/ijms27104179
• Dosing, Safety, and Tolerability of Extended-Release Tacrolimus in Pediatric and Young Adult Solid Organ Transplant Recipients.
  Pediatric transplantation · 2026 · Dang T, Hewlett J, McAteer J, et al.
  PMID 42175811DOI 10.1111/petr.70349
• Comparative efficacy of pediatric atopic dermatitis treatments: a network meta-analysis highlighting dupilumab and pimecrolimus for SCORAD and EASI improvement.
  Frontiers in immunology · 2026 · Yang L, Hu R, Wang Y, et al.
  PMID 42148141DOI 10.3389/fimmu.2026.1676852
• Iatrogenic immunodeficiency-associated polymorphic lymphoproliferative disorder resulting in complete remission after tacrolimus withdrawal in systemic lupus erythematosus: a case report.
  Modern rheumatology case reports · 2026 · Yoshida M, Mizushima I, Ikeda H, et al.
  PMID 42139076DOI 10.1093/mrcr/rxag038
• Continuous Subcutaneous Ketamine Infusion May Induce Tacrolimus and Sirolimus Clearance: A Case Report.
  Pharmacotherapy · 2026 · Stojanova J, Murnion B, Burrows F, et al.
  PMID 42115000DOI 10.1002/phar.70150
• Chitosan nanoparticles-incorporated polylactic acid/tacrolimus nanofiber composite membrane for tracheal scar inhibition and tracheal wound healing promotion.
  International journal of biological macromolecules · 2026 · Lv G, Feng S, Sang S, et al.
  PMID 42107578DOI 10.1016/j.ijbiomac.2026.152469

The 10 most recently updated of 1,596 ClinicalTrials.gov registrations naming Tacrolimus as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Stem Cell Transplantation for Participants With Germline RUNX1 Associated Blood Cancers
  Not yet recruiting · Phase 2 · Interventional · 98 enrolled · National Cancer Institute (NCI)
  NCT07524530updated 2026-06-12
• A Study to Learn More About the Effects and Safety of Felzartamab Infusions in Adults With Primary Membranous Nephropathy (PMN)
  Recruiting · Phase 3 · Interventional · 180 enrolled · Biogen
  NCT06962800updated 2026-06-12
• Phase 2 Study of Rapcabtagene Autoleucel in Myositis
  Active not recruiting · Phase 2 · Interventional · 21 enrolled · Novartis Pharmaceuticals
  NCT06665256updated 2026-06-11
• Drug-gene-nutraceutical Interactions of Cannabidiol and Tacrolimus
  Completed · Phase 1 · Interventional · 57 enrolled · Indiana University
  NCT05490511updated 2026-06-10
• Sorafenib, Busulfan and Fludarabine in Treating Patients With Recurrent or Refractory Acute Myeloid Leukemia Undergoing Donor Stem Cell Transplant
  Active not recruiting · Phase 1 · Phase 2 · Interventional · 74 enrolled · M.D. Anderson Cancer Center
  NCT03247088updated 2026-06-10
• Early Signals of the Transition From Immune Quiescence to Activation in the Liver Allograft Microenvironment and in the Circulation
  Recruiting · Phase 2 · Interventional · 100 enrolled · National Institute of Allergy and Infectious Diseases (NIAID)
  NCT07549503updated 2026-06-09
• Automated Total Marrow and Lymphoid Irradiation for Allogeneic Hematopoietic Cell Transplant
  Not yet recruiting · Phase 2 · Interventional · 30 enrolled · Stanford University
  NCT07634536updated 2026-06-09
• Tocilizumab in Lung Transplantation
  Recruiting · Phase 2 · Interventional · 350 enrolled · National Institute of Allergy and Infectious Diseases (NIAID)
  NCT06033196updated 2026-06-09
• Screening for Subclinical Antibody Mediated Rejection and Efficacy of Belatacept in the Context of de Novo Donor Specific Antibody After Kidney Transplantation (BELA-M-R)
  Not yet recruiting · Phase 2 · Phase 3 · Interventional · 290 enrolled · University Hospital, Rouen
  NCT06291103updated 2026-06-09
• Human Lysozyme Goat Milk for the Prevention of Graft Versus Host Disease in Patients With Blood Cancer Undergoing a Donor Stem Cell Transplant
  Active not recruiting · Phase 1 · Interventional · 52 enrolled · City of Hope Medical Center
  NCT04177004updated 2026-06-08

CPIC-curated drug–gene pairs for Tacrolimus. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

• CYP3A4CPIC C (provisional)ClinPGx 2A
• CYP3A5CPIC AClinPGx 1A
  CYP3A5 and Tacrolimus

Ranked by 2D fingerprint (Tanimoto) similarity over PubChem structures. Structural proximity only — not a claim of therapeutic equivalence.

• AzithromycinMacrolide Antimicrobial79%
• FosinoprilAngiotensin Converting Enzyme Inhibitor78%
• TiotropiumAnticholinergic78%
• ClarithromycinMacrolide Antimicrobial77%
• ErythromycinMacrolide75%
• RamiprilAngiotensin Converting Enzyme Inhibitor75%

Frequently asked questions

How does Tacrolimus work?

Tacrolimus binds to an intracellular protein, FKBP-12. A complex of tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin (a ubiquitous mammalian intracellular enzyme) is then formed, after which the phosphatase activity of calcineurin is inhibited.

What is Tacrolimus used for?

According to FDA labeling, Tacrolimus carries indications including: Tacrolimus capsules are calcineurin-inhibitor immunosuppressant indicated for the prophylaxis of organ rejection in adult patients receiving allogeneic liver, kidney or heart transplants and pediatric patients receiving allogeneic liver transplants in combination with other immunosuppressants. ( 1.1 ) 1.1 Prophylaxis of Organ Rejection in Kidney, Liver or Heart Transplant Tacrolimus capsules are indicated for the prophylaxis of organ rejection, in adult patients receiving allogeneic kidney transplant [ see Clinical Studies (14.1) ] , liver transplants [ see Clinical Studies (14.2) ] and heart transplant [ see Clinical Studies (14.3) ] , and pediatric patients receiving allogeneic liver transplants [ see Clinical Studies (14.2) ] in combination with other immunosuppressants.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Tacrolimus?

Tacrolimus is classified as Agents for dermatitis, excluding corticosteroids, Calcineurin inhibitors, Enzyme Inhibitors, Cellular Growth Phase Arrest, Decreased Cytokine Production, Decreased T Lymphocyte Production.

What are the brand names for Tacrolimus?

Tacrolimus is marketed under brand names including Astagraf, Envarsus, Prograf.

What are the contraindications for Tacrolimus?

Tacrolimus labeling lists contraindications including: Tacrolimus capsules are contraindicated in patients with a hypersensitivity to tacrolimus. Tacrolimus injection is contraindicated in patients with a hypersensitivity to HCO-60 (polyoxyl 60 hydrogenated castor oil).. Always consult the full prescribing information and a clinician.