Overview
Tacrolimus (also FK-506 or Fujimycin) is an immunosuppressive drug whose main use is after organ transplant to reduce the activity of the patient's immune system and so the risk of organ rejection. It is also used in a topical preparation in the treatment of severe atopic dermatitis, severe refractory uveitis after bone marrow transplants, and the skin condition vitiligo. It was discovered in 1984 from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis. Tacrolimus is chemically known as a macrolide. It reduces peptidyl-prolyl isomerase activity by binding to the immunophilin FKBP-12 (FK506 binding protein) creating a new complex. This FKBP12-FK506 complex inhibits calcineurin which inhibits T-lymphocyte signal transduction and IL-2 transcription.
Indication
Immediate-release formulations of tacrolimus are 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. Extended-release formulations of tacrolimus are indicated for the prophylaxis of organ rejection in adult and pediatric patients receiving kidney transplants, in combination with other immunosuppressants, and may be used in patients converted from immediate-release formulations. Topical tacrolimus ointment is indicated as second-line therapy for short-term and non-continuous treatment of moderate-to-severe atopic dermatitis in non-immunocompromised adults and children who have failed to respond adequately to other topical treatments or for whom alternative treatments are not advisable. Both available strengths are indicated in adult patients, while only the lower strength (0.03%) formulation is indicated in pediatric patients between 2 and 15 years of age.
Associated Conditions
- Graft-versus-host Disease (GVHD)
- Heart Transplant Rejection
- Kidney Transplant Rejection
- Liver Transplant Rejection
- Lung Transplant Rejection
- Oral Lichen Planus
- Psoriasis
- Pyoderma Gangrenosum
- Rheumatoid Arthritis
- Severe Atopic Dermatitis
- Vitiligo
- Moderate Atopic dermatitis
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2025/07/03 | Not Applicable | Completed | Wuhan Children's Hospital | ||
2025/05/30 | Phase 1 | Not yet recruiting | City of Hope Medical Center | ||
2025/05/08 | Phase 3 | Recruiting | |||
2025/03/28 | Not Applicable | Recruiting | Xijing Hospital | ||
2025/03/17 | Early Phase 1 | ENROLLING_BY_INVITATION | Dr ayesha wahid | ||
2025/03/12 | Phase 2 | Recruiting | |||
2025/02/14 | Phase 2 | Not yet recruiting | |||
2025/02/07 | Phase 2 | Recruiting | City of Hope Medical Center | ||
2025/02/04 | Phase 2 | Recruiting | |||
2024/11/22 | Phase 4 | Not yet recruiting |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| Sandoz Inc | 0781-2104 | ORAL | 5 mg in 1 1 | 6/20/2019 | |
| Mylan Institutional Inc. | 51079-817 | ORAL | 0.5 mg in 1 1 | 12/27/2023 | |
| Ascend Laboratories, LLC | 67877-279 | ORAL | 1 mg in 1 1 | 3/28/2023 | |
| Biocon Pharma Inc. | 70377-015 | ORAL | 1 mg in 1 1 | 10/7/2021 | |
| Astellas Pharma US, Inc. | 0469-0617 | ORAL | 1 mg in 1 1 | 5/31/2022 | |
| Accord Healthcare Inc. | 16729-421 | TOPICAL | 0.3 mg in 1 g | 3/17/2021 | |
| Panacea Biotec Limited | 43817-423 | ORAL | 5 mg in 1 1 | 12/25/2020 | |
| Sincerus Florida, LLC | 72934-4173 | TOPICAL | 0.1 g in 100 g | 5/9/2019 | |
| Veloxis Pharmaceuticals, Inc | 68992-3040 | ORAL | 4 mg in 1 1 | 7/26/2023 | |
| Accord Healthcare Inc. | 16729-041 | ORAL | 0.5 mg in 1 1 | 1/5/2024 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
Authorised | 7/18/2014 | ||
Authorised | 4/23/2007 | ||
Authorised | 2/27/2002 | ||
Authorised | 5/15/2009 |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| TACROCIN 5- TACROLIMUS CAPSULE USP 5 MG | SIN16157P | CAPSULE, GELATIN COATED | 5 mg | 4/21/2021 | |
| TACROCIN 1- TACROLIMUS CAPSULE USP 1 MG | SIN16158P | CAPSULE, GELATIN COATED | 1 mg | 4/21/2021 | |
| TACROLIMUS–TEVA PROLONGED RELEASE HARD CAPSULE 5MG | SIN16160P | CAPSULE, EXTENDED RELEASE | 5.0 mg | 4/21/2021 | |
| Advagraf Prolonged Release Hard Capsules 0.5 mg | SIN14133P | CAPSULE, EXTENDED RELEASE | 0.5 mg | 4/16/2012 | |
| TACROLIMUS SANDOZ CAPSULE 0.5 MG | SIN15673P | CAPSULE, GELATIN COATED | 0.5 mg | 4/25/2019 | |
| PROTOPIC OINTMENT 0.1% | SIN12524P | OINTMENT | 0.10g/100g | 3/8/2004 | |
| Advagraf Prolonged Release Hard Capsules 1 mg | SIN14134P | CAPSULE, EXTENDED RELEASE | 1.0 mg | 4/16/2012 | |
| TACROLIMUS–TEVA PROLONGED RELEASE HARD CAPSULE 1MG | SIN16161P | CAPSULE, EXTENDED RELEASE | 1.0 mg | 4/21/2021 | |
| SALVADO 0.5 CAPSULE 0.5MG | SIN16457P | CAPSULE | 0.5mg | 3/30/2022 | |
| TACROCIN 0.5- TACROLIMUS CAPSULE USP 0.5 MG | SIN16159P | CAPSULE, GELATIN COATED | 0.5 mg | 4/21/2021 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| Tacrolimus Ointment | 国药准字H20223426 | 化学药品 | 软膏剂 | 6/28/2022 | |
| Tacrolimus Ointment | 国药准字H20253184 | 化学药品 | 软膏剂 | 1/14/2025 | |
| Tacrolimus Ointment | 国药准字H20249414 | 化学药品 | 软膏剂 | 11/15/2024 | |
| Tacrolimus Ointment | 国药准字H20249415 | 化学药品 | 软膏剂 | 11/15/2024 | |
| Tacrolimus Ointment | 国药准字H20253186 | 化学药品 | 软膏剂 | 1/14/2025 | |
| Tacrolimus Ointment | 国药准字H20234047 | 化学药品 | 软膏剂 | 8/22/2023 | |
| Tacrolimus Ointment | 国药准字H20233893 | 化学药品 | 软膏剂 | 6/30/2023 | |
| Tacrolimus Ointment | 国药准字H20234728 | 化学药品 | 软膏剂 | 12/29/2023 | |
| Tacrolimus Ointment | 国药准字H20163257 | 化学药品 | 软膏剂 | 4/28/2021 | |
| Tacrolimus Ointment | 国药准字HJ20181016 | 化学药品 | 软膏剂 | 3/12/2021 |
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| TACROZ FORTE OINTMENT 0.1% W/W | N/A | N/A | N/A | 6/28/2017 | |
| TACROLIMUS CAPSULES USP 1MG | N/A | N/A | N/A | 3/3/2017 | |
| TACROLIMUS CAPSULES USP 5MG | N/A | N/A | N/A | 10/24/2024 | |
| TACROLIMUS CAPSULES USP 0.5MG | N/A | N/A | N/A | 10/24/2024 | |
| TACROLIMUS CAPSULES USP 1MG | N/A | N/A | N/A | 10/24/2024 | |
| TACROLIMUS CAPSULES 5MG | N/A | N/A | N/A | 6/20/2018 | |
| REMUS OINTMENT 0.03%W/W | N/A | N/A | N/A | 7/16/2012 | |
| PROGRAF CAP 1MG | N/A | N/A | N/A | 4/21/1997 | |
| TACROCORD 0.5 CAPSULES 0.5MG | N/A | N/A | N/A | 6/17/2025 | |
| TACROCORD 5 CAPSULES 5MG | N/A | N/A | N/A | 6/17/2025 |
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| PROGRAF tacrolimus 1mg capsule blister pack | 58930 | Medicine | A | 8/25/1997 | |
| PROGRAF-XL tacrolimus 0.5 mg prolonged-release capsule blister pack | 158439 | Medicine | A | 3/31/2010 | |
| ADVAGRAF XL tacrolimus 0.5 mg prolonged-release capsule blister pack | 269212 | Medicine | A | 5/23/2016 | |
| ADVAGRAF XL tacrolimus 5 mg prolonged-release capsule blister pack | 269215 | Medicine | A | 5/23/2016 | |
| Talocran tacrolimus 0.5 mg capsules | 212315 | Medicine | A | 7/17/2013 | |
| Talocran tacrolimus 1 mg capsules | 212316 | Medicine | A | 7/17/2013 | |
| TACROLIMUS ACT tacrolimus 0.5 mg capsules blister pack | 224276 | Medicine | A | 5/27/2015 | |
| PROGRAF XL tacrolimus 3 mg prolonged-release capsules blister pack | 306500 | Medicine | A | 7/19/2019 | |
| PROGRAF-XL tacrolimus 5 mg prolonged-release capsule blister pack | 158444 | Medicine | A | 3/31/2010 | |
| PROGRAF tacrolimus 5mg capsule blister pack | 58931 | Medicine | A | 8/25/1997 |
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