| Drug ID: | Drug70 |
|---|---|
| Drug Name: | Tacrolimus |
| CID: | 445643 |
| DrugBank ID: | DB00864 |
| Modality: | Small Molecule |
| Groups: | approved|investigational |
| US Approved: | YES |
| Other Approved: | YES |
| Identifier: | NCT00643071, , NCT00514982, , NCT02954159, , NCT06867042, , NCT00347048 |
| Molecular Formula: | C44H69NO12 |
| Molecular Weight: | 804.0 g/mol |
| Isomeric SMILES: | C[C@@H]1C[C@@H]([C@@H]2[C@H](C[C@H]([C@@](O2)(C(=O)C(=O)N3CCCC[C@H]3C(=O)O[C@@H]([C@@H]([C@H](CC(=O)[C@@H](/C=C(/C1)\\C)CC=C)O)C)/C(=C/[C@@H]4CC[C@H]([C@@H](C4)OC)O)/C)O)C)OC)OC |
| Synonyms: | tacrolimus; 104987-11-3; Fujimycin; Prograf; Tsukubaenolide; Tacrolimus anhydrous; Protopic; Anhydrous Tacrolimus; Advagraf; Modigraf |
| Phase 0: | 14 |
| Phase 1: | 178 |
| Phase 2: | 466 |
| Phase 3: | 223 |
| Phase 4: | 390 |
| Description: | 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 interacts with and inhibits calcineurin thus inhibiting both T-lymphocyte signal transduction and IL-2 transcription. |
Molecular Structure
Knowledge Graph
| dtID | CID | Compound Name | Gene ID | Gene Name | Species | PubMed IDs | Action |
|---|---|---|---|---|---|---|---|
| dt593 | 445643 | Tacrolimus | 3558 | IL2 | Homo sapiens (human) | None | |
| dt594 | 445643 | Tacrolimus | 221785 | ZSCAN25 | Homo sapiens (human) | None | |
| dt595 | 445643 | Tacrolimus | 3290 | HSD11B1 | Homo sapiens (human) | None | |
| dt596 | 445643 | Tacrolimus | 1565 | CYP2D6 | Homo sapiens (human) | None | |
| dt597 | 445643 | Tacrolimus | 2609 | GAPDHP67 | Homo sapiens (human) | Inhibitor | |
| dt598 | 445643 | Tacrolimus | 79054 | TRPM8 | Homo sapiens (human) | Activator | |
| dt599 | 445643 | Tacrolimus | 2280 | FKBP1A | Homo sapiens (human) | None | |
| dt600 | 445643 | Tacrolimus | 6696 | SPP1 | Homo sapiens (human) | None | |
| dt601 | 445643 | Tacrolimus | 387082 | SUMO4 | Homo sapiens (human) | None |
- No data available
Phase Distribution
Phase Description
- Phase 0: Exploratory trials to assess drug behavior in humans
- Phase 1: Safety trials to determine safe dosage range
- Phase 2: Efficacy trials to evaluate therapeutic effects
- Phase 3: Large-scale trials to confirm efficacy and safety
- Phase 4: Post-marketing surveillance for long-term safety and efficacy
| Trial ID | Title | Phase | Status | Sponsor | Indications | Interventions | |
|---|---|---|---|---|---|---|---|
| NCT00347048 | Tacrolimus (FK506) Study in Moderate to Severe Refractory Ulcerative Colitis Patients | PHASE3 | COMPLETED | Astellas Pharma Inc | Ulcerative Colitis | DRUG: tacrolimus|DRUG: Placebo | Details |
| NCT00643071 | Tacrolimus (FK506) P-III, Open-label Study in Refractory Ulcerative Colitis Patients | PHASE3 | COMPLETED | Astellas Pharma Inc | Ulcerative Colitis | DRUG: Tacrolimus | Details |
| NCT00514982 | Medical Treatment of Colitis in Patients With Hermansky-Pudlak Syndrome | PHASE2 | WITHDRAWN | National Institute of Allergy and Infectious Diseases (NIAID) | Hermanski-Pudlak Syndrome|Colitis|Cytokines|Lymph… | DRUG: Mesalamine|DRUG: Infliximab|DRUG: Corticost… | Details |
| NCT06867042 | Tacrolimus Lipid Suspension for Enema in Adult Subjects with Mild to Moderately Active Left-sided/Distal Ulcerative Colitis Who Had an Inadequate Response to the Treatment | PHASE2 | NOT_YET_RECRUITING | Jina Pharmaceuticals Inc. | Ulcerative Colitis (UC)|Ulcerative Colitis, Activ… | DRUG: Tacrolimus Lipid Suspension for enema|DRUG:… | Details |
| NCT02954159 | Vedolizumab Monotherapy Vs Combination Therapy With Tacrolimus in UC | PHASE3 | TERMINATED | Medical College of Wisconsin | Ulcerative Colitis | DRUG: Tacrolimus|DRUG: Vedolizumab|OTHER: Placebo | Details |
| CTRI/2021/10/037641 | An open label study to compare the efficacy and safety of tofacitinib compared to corticosteroids for inducing remission in moderately severe active ulcerative colitis | PHASE4 | Recruiting | Dayanand Medical College and Hospital Ludhiana | Disease.2. Total mayo clinic score <6 or >9. 3.… | Health Condition 1: K51- Ulcerative colitis | Details |
| NCT03204136 | Tacrolimus Versus Methotrexate as Rescue Therapy for Refractory Inflammatory Bowel Disease: an Open-label, Retrospective Study | Not Available | Not recruiting | Key Laboratory of Gastroenterology and Hepatology, Ministry of Health, China | Inflammatory Bowel Diseases;Inflammatory Bowel Di… | None | Details |
| NCT01418131 | Rectal Tacrolimus in the Treatment of Resistant Ulcerative Proctitis | PHASE4 | COMPLETED | The University of Western Australia | Ulcerative Colitis | DRUG: Rectal tacrolimus|DRUG: Placebo | Details |
| Disease ID | Disease Name | Definition | Category | Related Drugs | Mechanism | |
|---|---|---|---|---|---|---|
| No data available | ||||||
| Strategy ID | Therapeutic Strategy | Synonyms | Related Drugs | Mechanism | |
|---|---|---|---|---|---|
| S02 | Immunosuppression | Classic immunosuppressive drugs | azathioprine; 6-mercaptopurine; methotrexate; ciclosporin-A; tacrolimus | Ciclosporin-A and tacrolimus bind to specific intracellular… | Details |
Effectiveness and safety of rectal tacrolimus in patients with ulcerative colit…
PMID: 40205922
Year: 2025
Relationship Type:
Treatment
Score: 6.5
INTRODUCTION: Data about the efficacy of topical therapy with tacrolimus in patients with ulcerative colitis (UC) are scarce. Therefore, this study a…
Effectiveness of tacrolimus therapy in refractory ulcerative colitis compared t…
PMID: 39747885
Year: 2025
Relationship Type:
Treatment
Score: 6.5
There is insufficient evidence comparing the outcomes of tacrolimus-based remission induction therapy with infliximab in refractory ulcerative coliti…
The Role of Topical Tacrolimus in the Management of Inflammatory Bowel Disease:…
PMID: 39337004
Year: 2024
Relationship Type:
Treatment
Score: 6.5
Management of ulcerative colitis and Crohn's disease, the main subtypes of inflammatory bowel disease (IBD), focuses on the induction and maintenance…
Tacrolimus-Associated Terminal Ileitis After Kidney Transplantation, Mimicking …
PMID: 38368132
Year: 2024
Relationship Type:
Treatment
Score: 6.5
The onset of gastroduodenal ulcers is a frequent complication after transplantation, whereas cases of intestinal ulcers are sporadic and poorly descr…
Drug Interaction Between Tacrolimus and Paxlovid (Nirmatrelvir/Ritonavir) in an…
PMID: 38034448
Year: 2023
Relationship Type:
Adverse Effect
Score: 6.5
The coronavirus disease of 2019 (COVID-19) led to a worldwide pandemic. The emergency use of a combination of nirmatrelvir/ritonavir (paxlovid) was a…
Efficacy and Safety of Tacrolimus or Infliximab Therapy in Children and Young A…
PMID: 37477885
Year: 2023
Relationship Type:
Treatment
Score: 6.5
INTRODUCTION: One-third of children and young adults admitted for management of acute severe colitis (ASC) fail intravenous corticosteroids. Inflixim…
Systemic calcineurin inhibitors tacrolimus and voclosporin: A review of off-lab…
PMID: 37307993
Year: 2024
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Systemic calcineurin inhibitors, cyclosporine, tacrolimus, and voclosporin, have been utilized in various dermatologic conditions. Althou…
Oral Tacrolimus in Steroid Refractory and Dependent Pediatric Ulcerative Coliti…
PMID: 37184447
Year: 2023
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: There are limited treatment options for children with steroid-refractory or dependent ulcerative colitis (UC). A few observational studie…
Combination of Lactobacillus plantarum improves the effects of tacrolimus on co…
PMID: 36992690
Year: 2023
Relationship Type:
Treatment
Score: 6.5
The gut microbiome has been considered to play an important role in inflammatory bowel disease (IBD). Our previous study reported that tacrolimus-alt…
Network meta-analysis and cost-effectiveness analysis of infliximab, cyclospori…
PMID: 36595876
Year: 2022
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Assess the efficiency and cost-effectiveness of infliximab, cyclosporine and tacrolimus for the treatment of ulcerative colitis (UC). MET…
Thiopurine naivety at tacrolimus induction is a predictor of long-term remissio…
PMID: 36128954
Year: 2023
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: The short-term efficacy of tacrolimus (Tac) for steroid-dependent and steroid-resistant refractory ulcerative colitis (UC) has been demon…
Lymphocyte to monocyte ratio and serum albumin changes predict tacrolimus thera…
PMID: 35945329
Year: 2022
Relationship Type:
Treatment
Score: 6.5
Tacrolimus therapy for ulcerative colitis is ineffective in certain patients; these patients require biologics or colectomy. We examined the ability …
Risk Factors for Nephrotoxicity due to Tacrolimus Therapy for Ulcerative Colitis
PMID: 35705006
Year: 2022
Relationship Type:
Treatment
Score: 6.5
BACKGROUND AND AIMS: The calcineurin inhibitor tacrolimus is reportedly effective for moderate/severe ulcerative colitis (UC); however, it is also re…
Long-lasting renal dysfunction following tacrolimus induction therapy in ulcera…
PMID: 35692680
Year: 2022
Relationship Type:
Treatment
Score: 6.5
Although tacrolimus (TAC) has remarkable effects in ulcerative colitis (UC) patients when given as remission induction therapy, some can develop rena…
Tacrolimus-binding protein FKBP8 directs myosin light chain kinase-dependent ba…
PMID: 35537812
Year: 2023
Relationship Type:
Treatment
Score: 6.5
OBJECTIVE: Intestinal barrier loss is a Crohn's disease (CD) risk factor. This may be related to increased expression and enzymatic activation of myo…
Tacrolimus (FK506) for induction of remission in corticosteroid-refractory ulce…
PMID: 35388476
Year: 2022
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: There are a limited number of treatment options for people with corticosteroid-refractory ulcerative colitis. Animal models of inflammato…
Induction of remission with tacrolimus in a patient with severe acute, cortison…
PMID: 35033015
Year: 2022
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Therapy regimens used in patients with inflammatory Bowel Disease (IBD) have been associated with enhanced risk of viral infections or vi…
Tacrolimus as rescue therapy for steroid-dependent/steroid-refractory ulcerativ…
PMID: 34971402
Year: 2021
Relationship Type:
Treatment
Score: 6.5
INTRODUCTION: Between 20% and 40% of patients with severe ulcerative colitis (UC) are either steroid-refractory UC (SRUC) or steroid-dependent UC (SD…
Intravenous tacrolimus is a superior induction therapy for acute severe ulcerat…
PMID: 34949172
Year: 2021
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Intravenous corticosteroid is the mainstay for managing acute severe ulcerative colitis, but one-third of patients do not respond to intr…
Early serum albumin changes in patients with ulcerative colitis treated with ta…
PMID: 34168412
Year: 2021
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Oral tacrolimus is a therapeutic agent for moderate to severe steroid-dependent or resistant ulcerative colitis (UC), but remission induc…