TACROLIMUS
Tacrolimus extended-release capsules are a calcineurin-inhibitor immunosuppressant indicated for the prophylaxis of organ rejection in adult kidney transplant recipients. The formulation is intended for use in combination with other immunosuppressive agents and must be swallowed intact. By suppressing T-lymphocyte activation and proliferation, the medication prevents the immune-mediated rejection of the transplanted organ.
How TACROLIMUS Works
Tacrolimus exerts its immunosuppressive effect by binding to the intracellular protein FKBP-12, forming a complex that inhibits the phosphatase activity of calcineurin. This inhibition prevents the dephosphorylation and nuclear translocation of transcription factors, such as the nuclear factor of activated T-cells (NF-AT). Consequently, the expression of various cytokines (including IL-2, IL-4, and interferon-gamma) is suppressed, leading to the inhibition of T-lymphocyte activation and proliferation, as well as T-helper-cell-dependent B-cell responses.
Details
- Status
- Prescription
- First Approved
- 2009-08-10
- Routes
- ORAL, TOPICAL, INJECTION
- Dosage Forms
- CAPSULE, OINTMENT, INJECTABLE, CAPSULE, EXTENDED RELEASE
TACROLIMUS Approval History
What TACROLIMUS Treats
18 FDA approvalsOriginally approved for its first indication in 2009 . Covers 18 distinct patient populations.
- Other (18)
Other
(18 approvals)- • Approved indication (Aug 2009)Label Letter
- • Approved indication (May 2010)
- • Approved indication (Jul 2010)
- • Approved indication (Sep 2010)
- • Approved indication (Aug 2011)
- • Approved indication (Sep 2012)
- • Approved indication (Jul 2014)
- • Approved indication (Sep 2014)Letter
- • Approved indication (Aug 2017)Letter
- • Approved indication (Nov 2017)
- • Approved indication (Apr 2018)
- • Approved indication (Jan 2019)
- • Approved indication (Nov 2020)
- • Approved indication (Nov 2020)
- • Approved indication (Apr 2023)
- • Approved indication (Oct 2023)
- • Approved indication (Jan 2024)
- • Approved indication (Feb 2025)
TACROLIMUS Boxed Warning
MALIGNANCIES AND SERIOUS INFECTIONS IN TRANSPLANT PATIENTS; AND INCREASED MORTALITY IN FEMALE LIVER TRANSPLANT PATIENTS Increased risk for developing serious infections and malignancies with tacrolimus extended-release capsulest or other immunosuppressants that may lead to hospitalization or death. [see Warnings and Precautions ( 5.1 , 5.2 )] Increased mortality in female liver transplant patients with tacrolimus extended-release capsulest. Tacrolimus extended-release capsulest is not approved f...
WARNING: MALIGNANCIES AND SERIOUS INFECTIONS IN TRANSPLANT PATIENTS; AND INCREASED MORTALITY IN FEMALE LIVER TRANSPLANT PATIENTS Increased risk for developing serious infections and malignancies with tacrolimus extended-release capsulest or other immunosuppressants that may lead to hospitalization or death. [see Warnings and Precautions ( 5.1 , 5.2 )] Increased mortality in female liver transplant patients with tacrolimus extended-release capsulest. Tacrolimus extended-release capsulest is not approved for use in liver transplantation. [see Warnings and Precautions ( 5.3 )] WARNING: MALIGNANCIES AND SERIOUS INFECTIONS IN TRANSPLANT PATIENTS; and INCREASED MORTALITY IN FEMALE LIVER TRANSPLANT PATIENTS See full prescribing information for complete boxed warning. Increased risk for developing serious infections and malignancies with with tacrolimus extended-release capsules or other immunosuppressants that may lead to hospitalization or death. ( 5.1 , 5.2 ) Increased mortality in female liver transplant patients with with tacrolimus extended-release capsules. Not approved for use in liver transplantation. ( 5.3 )
TACROLIMUS Target & Pathway
ProTarget
TACROLIMUS Competitive Set
ProThree rings of competition based on shared molecular targets and treated indications.
MoA expansion candidates
Same target(s), different indications — where else is this mechanism being explored?
Filters applied: drops same-active-ingredient (505(b)(2) reformulations), route-mismatch (topical vs systemic), and cross-therapeutic-area matches in same-indication rings.
Clinical Trial Registry
370 trials| Trial | Sponsor ID | Phase | Status | Title |
|---|---|---|---|---|
| NCT07524530 | 10002233 002233-C | Ph 2 | not yet recruiting | Stem Cell Transplantation for Participants With Germline RUNX1 Associated Blood Cancers |
| NCT05088356 | IRB-60439 NCI-2021-12228 | Ph 1 | active not recruiting | Reduced Intensity Allogeneic HCT in Advanced Hematologic Malignancies w/T-Cell Depleted Graft |
| NCT07582172 | 25663 NCI-2026-03208, 25663 | Ph 2 | not yet recruiting | Total Marrow and Lymphoid Irradiation in Combination With Fludarabine and Melphalan as Conditioning for Allogeneic Peripheral Blood Stem Cell Hematopoietic Cell Transplant in Older Patients With Refractory and Relapsed Acute Myeloid Leukemia and High-risk Myelodysplastic Syndrome |
| NCT07204275 OLYMPUS | VX24-AIS-D10 2025-521661-27-00 | Ph 2, Ph 3 | recruiting | Evaluation of Efficacy, Safety, and Tolerability of Povetacicept in Participants With Primary Membranous Nephropathy (pMN) |
| NCT06996119 | 23822 NCI-2025-03603, 23822 | Ph 1 | recruiting | Emapalumab With Post-Transplant Cyclophosphamide, Tacrolimus and Mycophenolate Mofetil for the Prevention of Graft-versus-Host Disease After Donor Reduced-Intensity Hematopoietic Cell Transplant |
| NCT05027945 | 10000404 000404-C | Ph 2 | recruiting | A Phase II Study of Allogeneic Hematopoietic Stem Cell Transplant for Subjects With VEXAS (Vacuoles, E1 Enzyme, X-linked, Autoinflammatory, Somatic) Syndrome |
| NCT01861106 | 130132 13-C-0132 | Ph 2 | recruiting | Allogeneic Hematopoietic Stem Cell Transplant for GATA2 Mutations |
| NCT07566377 | 26-168 | Ph 2 | recruiting | Cord Blood Transplantation in Children and Young Adults With Blood Cancer |
| NCT06962800 PROMINENT | 299PN301 2024-519232-16-00 | Ph 3 | recruiting | A Study to Learn More About the Effects and Safety of Felzartamab Infusions in Adults With Primary Membranous Nephropathy (PMN) |
| NCT03670966 | RG1003349 10060, P30CA015704 | Ph 1, Ph 2 | recruiting | 211At-BC8-B10 Followed by Donor Stem Cell Transplant in Treating Patients With Relapsed or Refractory High-Risk Acute Leukemia or Myelodysplastic Syndrome |
| NCT03816332 results posted | NCI-2019-00239 NCI-2019-00239, ETCTN10214 | Ph 1 | active not recruiting | Tacrolimus, Nivolumab, and Ipilimumab in Treating Kidney Transplant Recipients With Selected Unresectable or Metastatic Cancers |
| NCT06195891 | 23343 NCI-2023-08816, 23343 | Ph 1 | recruiting | Orca-T Following Chemotherapy and Total Marrow and Lymphoid Irradiation for the Treatment of Acute Myeloid Leukemia, Acute Lymphoblastic Leukemia or Myelodysplastic Syndrome |
| NCT06807606 | 2024-1605 NCI-2025-00794 | Ph 2 | recruiting | Optimized Cord Blood Transplantation for the Treatment of Patients With High-risk Hematologic Malignancies Who Have Relapsed After First Allogeneic Stem Cell Transplantation |
| NCT07412470 FREXERA | EFC18554 2025-521521-33-00 | Ph 2, Ph 3 | recruiting | A Study to Investigate the Efficacy and Safety of Frexalimab Versus Tacrolimus in Adults Undergoing Kidney Transplantation |
| NCT07548983 | STUDY00028015 NCI-2025-09157, STUDY00028015 | Ph 1 | not yet recruiting | Ruxolitinib With Azacitidine Maintenance for the Treatment of Patients With Acute Myeloid Leukemia Undergoing Reduced Intensity Allogeneic Stem Cell Transplantation |
| NCT07302776 | IRB-82367 | Ph 1 | not yet recruiting | TACrolimus Targeted Immunosuppression Cessation in ALlogeneic HCT |
| NCT07493538 | 2025LS162 | Ph 2 | recruiting | MT2025-35 Allogeneic Hematopoietic Stem Cell Transplantation Using Reduced Intensity Conditioning Treosulfan and Fludarabine, With Post-Transplant Cytoxan (PTCy) for the Treatment of Hematological Diseases |
| NCT07349771 | MC230810 24-009803 | Ph 2 | not yet recruiting | Axatilimab Plus Standard of Care Therapy for the Prevention of Graft Versus Host Disease Following Allogeneic Hematopoietic Stem Cell Transplantation in Patients With Hematologic Cancer, ABRAXAS Trial |
| NCT06828796 | NSH 1420 | Ph 2 | recruiting | Early Use of Tacrolimus in HLA-Mismatched Haploidentical Allogeneic Hematopoietic Transplantation With Post-Transplant Cyclophosphamide |
| NCT04859946 | 2020-0971 NCI-2021-02784, 2020-0971 | Ph 2 | active not recruiting | Itacitinib for the Prevention of Graft Versus Host Disease |
| NCT04177004 | 19214 NCI-2019-06454, 19214 | Ph 1 | suspended | Human Lysozyme Goat Milk for the Prevention of Graft Versus Host Disease in Patients With Blood Cancer Undergoing a Donor Stem Cell Transplant |
| NCT03856216 results posted | 2018-0860 NCI-2019-00531, 2018-0860 | Ph 2 | terminated | Inotuzumab Ozogamicin and Chemotherapy in Treating Patients With Leukemia or Lymphoma Undergoing Stem Cell Transplantation |
| NCT01384513 results posted | 11D.247 2011-31, JT 1795 | Ph 2 | completed | A Two-Step Approach to Reduced Intensity Bone Marrow Transplant for Patients With Hematological Malignancies |
| NCT04384692 | RG1006507 NCI-2020-01626, 10093 | Ph 2 | active not recruiting | Peritransplant Ruxolitinib for Patients With Primary and Secondary Myelofibrosis |
| NCT03640026 GLITTER | CHD045-17 | Ph 4 | terminated | Glucose Disorders Induced by Tacrolimus on Pre Transplantation Endstage Renal Disease Patients |
| NCT00792948 results posted | NCI-2009-00800 NCI-2009-00800, S0805 | Ph 2 | active not recruiting | Combination Chemotherapy With or Without Donor Stem Cell Transplant in Treating Patients With Acute Lymphoblastic Leukemia |
| NCT06084780 TRANSCAPE | CASE7Z23 | Ph 2 | not yet recruiting | Intestinal & Multivisceral Transplantation for Unresectable Mucinous Carcinoma Peritonei (TRANSCAPE) |
| NCT05736419 | 23-009 | Ph 2 | recruiting | A Study of Immune Suppression Treatment for People With Sickle Cell Disease or β-Thalassemia Who Are Going to Receive an Allogeneic Hematopoietic Cell Transplantation (HCT) |
| NCT06478017 | DAIT RTB-013 | Ph 2 | recruiting | Belatacept in Heart Transplantation |
| NCT04629248 MAJESTY | WA41937 2020-003233-38, 2023-506525-11-00 | Ph 3 | active not recruiting | A Study Evaluating the Efficacy and Safety of Obinutuzumab in Participants With Primary Membranous Nephropathy |
| NCT02891603 results posted | MCC-18783 5R01HL133823-02 | Ph 1, Ph 2 | completed | A Phase I/II GVHD Prevention Trial Combining Pacritinib With Sirolimus-Based Immune Suppression |
| NCT03605927 | MCC-19305 | Ph 1 | completed | CD40-L Blockade for Prevention of Acute Graft-Versus-Host Disease |
| NCT02918292 CHAMP results posted | BMT CTN 1502 2U10HL069294-11, 5U24CA076518 | Ph 2 | completed | Optimizing Haploidentical Aplastic Anemia Transplantation (BMT CTN 1502) |
| NCT02333162 | IRB14-0709 NCI-2014-02469, IRB14-0709 | Ph 1 | suspended | Intensity Modulated Total Marrow Irradiation, Fludarabine Phosphate, and Melphalan in Treating Patients With Relapsed Hematologic Cancers Undergoing a Second Donor Stem Cell Transplant |
| NCT04339101 results posted | 19576 NCI-2020-01722, 19576 | Ph 2 | completed | Itacitinib, Tacrolimus, and Sirolimus for the Prevention of GVHD in Patients With Acute Leukemia, Myelodysplastic Syndrome, or Myelofibrosis Undergoing Reduced Intensity Conditioning Donor Stem Cell Transplantation |
| NCT02251821 results posted | 9033 NCI-2014-01882, 9033 | Ph 2 | completed | JAK Inhibitor Before Donor Stem Cell Transplant in Treating Patients With Primary or Secondary Myelofibrosis |
| NCT01659606 | 12-950 IRB-P00003466 | Ph 2 | active not recruiting | Radiation- and Alkylator-free Bone Marrow Transplantation Regimen for Patients With Dyskeratosis Congenita |
| NCT03321656 | 42753 | Ph 2, Ph 3 | recruiting | Impact of Envarsus XR® on Kidney Biopsy Subclinical Rejection and Blood Immunologic Profile |
| NCT03663335 CIRRUS I results posted | CCFZ533A2201 2017-003607-22 | Ph 2 | completed | Study of Efficacy, Safety, Tolerability, Pharmacokinetic (PK) and Pharmacodynamic (PD) of an Anti-CD40 Monoclonal Antibody, CFZ533, in Kidney Transplant Recipients |
| NCT07214688 | Pro2025-0254 FLU-TBI-800-PTCY | Ph 2 | recruiting | Fludarabine and Intermediate-dose TBI Followed by PTCy in Patients Undergoing Allo Transplant for Heme Malignancies |
| NCT04904588 ACCESS | ACCESS | Ph 2 | active not recruiting | HLA-Mismatched Unrelated Donor Hematopoietic Cell Transplantation With Post-Transplantation Cyclophosphamide |
| NCT03663933 results posted | 180135 18-C-0135 | Ph 2 | active not recruiting | Allogeneic Hematopoietic Cell Transplantation for Disorders of T-cell Proliferation and/or Dysregulation |
| NCT01804634 | J12106 NA_00076243, 5P01CA225618-06 | Ph 2 | recruiting | Reduced Intensity Haploidentical BMT for High Risk Solid Tumors |
| NCT03970096 | RG1005364 9749, NCI-2019-03188 | Ph 2 | recruiting | Graft Versus Host Disease-Reduction Strategies for Donor Blood Stem Cell Transplant Patients With Acute Leukemia or Myelodysplastic Syndrome (MDS) |
| NCT05622318 | PRO00046962 | Ph 2 | active not recruiting | De-escalated Cyclophosphamide (PTCy) and Ruxolitinib for Graft-versus-Host Disease (GVHD) Prophylaxis |
| NCT06872333 | 2024LS140 | Ph 2 | recruiting | Allo HSCT for High Risk Hemoglobinopathies |
| NCT06345495 | 2023-0899 NCI-2024-02814 | Ph 2 | recruiting | High Dose Ruxolitinib and Allogeneic Stem Cell Transplantation in Myelofibrosis Patients With Splenomegaly |
| NCT04965597 | BMTCTN1904 2U10HL069294-11, RG1121820 | Ph 2 | completed | Treosulfan-Based Conditioning Regimen Before a Blood or Bone Marrow Transplant for the Treatment of Bone Marrow Failure Diseases (BMT CTN 1904) |
| NCT06638879 | 2023-0687 | Ph 1 | completed | Tacrolimus Toothpaste for Management of Oral Chronic Graft vs. Host Disease (cGVHD) |
| NCT05707377 ALMOND | BGB-3111-309 2022-501147-32-00, CTR20230546 | Ph 2, Ph 3 | active not recruiting | A Study to Examine the Efficacy and Safety of Zanubrutinib Given to Adults With Primary Membranous Nephropathy |
Showing 50 of 370 trials
Active Pipeline
Ongoing clinical trials by development phase
Key Completed Trials
Completed studies with published results, ranked by significance
Trial Timeline
Full development history with FDA approval milestones
Understanding FDA Approval Types
| Count | Type | What it means |
|---|---|---|
| - | ORIG | Original approval - drug first enters market |
| - | SUPPL - Efficacy | New indication (new disease/condition approved) |
| - | SUPPL - Labeling | Label text changes (warnings, dosing updates) |
| - | SUPPL - Manufacturing | Production changes (new facility) |
| - | SUPPL - Chemistry | Formulation changes (new dosage strength) |
Green lines in the timeline show ORIG and Efficacy approvals - the clinically meaningful milestones.
TACROLIMUS FDA Label Details
Indications & Usage
FDA Label (PDF)Tacrolimus extended-release capsules is indicated for the prophylaxis of organ rejection in kidney transplant patients in combination with other immunosuppressants in adult patients who can swallow capsules intact [see Clinical Studies , ] . Pediatric use information is approved for Astellas Pharma US, Inc.'s ASTAGRAF XL (tacrolimus extended-release capsules). However, due to Astellas Pharma US, Inc.'s marketing exclusivity rights, this drug product is not labeled with that information. Tacrolimus extended-release capsules is a calcineurin-inhibitor immunosuppressant indicated for the prophyla...
WARNING: MALIGNANCIES AND SERIOUS INFECTIONS IN TRANSPLANT PATIENTS; AND INCREASED MORTALITY IN FEMALE LIVER TRANSPLANT PATIENTS Increased risk for developing serious infections and malignancies with tacrolimus extended-release capsulest or other immunosuppressants that may lead to hospitalization o...
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PROGRAF
Full clinical data, patents, trials, and competitive landscape for tacrolimus.
Data Sources
Data sourced from official FDA and NIH databases. Click links to verify on original sources.