| 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 |
Delivery of tacrolimus with cationic lipid-assisted nanoparticles for ulcerativ…
PMID: 29850666
Year: 2018
Relationship Type:
Treatment
Score: 6.3
Oral drug delivery with nanoparticles has demonstrated great potential for drugs with poor bioavailability. Efficient delivery is possible by overcom…
Tacrolimus therapy in moderate to subacute ulcerative proctocolitis: a large si…
PMID: 29588844
Year: 2018
Relationship Type:
Treatment
Score: 6.3
OBJECTIVE: To explore the 'real world' effectiveness of tacrolimus therapy for refractory ulcerative proctocolitis (UC). DESIGN: Retrospective cohort…
Outcome of tacrolimus and vedolizumab after corticosteroid and anti-TNF failure…
PMID: 29527316
Year: 2018
Relationship Type:
Treatment
Score: 6.3
BACKGROUND: Severe colitis flare from ulcerative colitis (UC) or Crohn's disease (CD) may be refractory to corticosteroids and antitumour necrosis fa…
Tacrolimus Dose Optimization Strategy for Refractory Ulcerative Colitis Based o…
PMID: 29393157
Year: 2018
Relationship Type:
Treatment
Score: 6.3
BACKGROUND: In the tacrolimus treatment for refractory ulcerative colitis (UC), dose adjustment is necessary because the required doses to keep appro…
Comparison of Safety and Efficacy of Tacrolimus versus Infliximab for Active Ul…
PMID: 29050007
Year: 2018
Relationship Type:
Treatment
Score: 6.3
BACKGROUND: This narrative review was to determine which medication, tacrolimus (TAC) or infliximab (IFX), is safer and more effective in the managem…
Medium to long-term efficacy and safety of oral tacrolimus in moderate to sever…
PMID: 28617029
Year: 2017
Relationship Type:
Treatment
Score: 6.3
BACKGROUND AND OBJECTIVE: Oral tacrolimus is an effective drug that induces clinical remission in patients with moderate to severe ulcerative colitis…
Rapid Induction Therapy with Oral Tacrolimus in Elderly Patients with Refractor…
PMID: 28411286
Year: 2017
Relationship Type:
Treatment
Score: 6.3
BACKGROUND Tacrolimus is reportedly effective for the treatment of refractory ulcerative colitis (UC). At our hospital, there has been an increase in…
EFFICACY OF TACROLIMUS FOR INDUCTION OF REMISSION IN PATIENTS WITH MODERATE-TO-…
PMID: 28327826
Year: 2017
Relationship Type:
Treatment
Score: 6.3
BACKGROUND: There is evidence that shows that calcineurin inhibitors may be useful for the treatment of severe ulcerative colitis. However, evidence …
A comparison of short-term therapeutic efficacy between infliximab and tacrolim…
PMID: 28222041
Year: 2017
Relationship Type:
Treatment
Score: 6.3
INTRODUCTION: Both infliximab (IFX) and tacrolimus (Tac) are effective for inducing clinical remission in patients with ulcerative colitis (UC). Howe…
ATP-binding cassette subfamily B member 1 1236C/T polymorphism significantly af…
PMID: 28135009
Year: 2017
Relationship Type:
Treatment
Score: 6.3
BACKGROUND AND AIM: Tacrolimus is now considered to be one of the main therapeutic options for refractory ulcerative colitis. Both cytochrome P-450 3…
Tacrolimus-associated Diffuse Gastrointestinal Ulcerations and Pathergy: A Case…
PMID: 28104141
Year: 2017
Relationship Type:
Treatment
Score: 6.3
Tacrolimus is a common immunosuppressive modality with a range of therapeutic applications, including for rheumatologic disease, nephrotic syndrome, …
The effect of CYP3A5 genetic polymorphisms on adverse events in patients with u…
PMID: 27717793
Year: 2017
Relationship Type:
Treatment
Score: 6.3
BACKGROUND: Tacrolimus is an immunosuppressive agent, used in the remission induction therapy of ulcerative colitis (UC). AIMS: We investigated the c…
Tacrolimus Exerts Only a Transient Effectiveness in Refractory Pediatric Crohn …
PMID: 27429426
Year: 2017
Relationship Type:
Treatment
Score: 6.3
OBJECTIVES: Tacrolimus is an immunosuppressive agent that has been proposed in the treatment of severe ulcerative colitis. The present study examined…
Comparison of the therapeutic efficacy and safety between tacrolimus and inflix…
PMID: 26818468
Year: 2016
Relationship Type:
Treatment
Score: 6.3
OBJECTIVE: Both tacrolimus (Tac) and infliximab (IFX) are effective for moderate-to-severe ulcerative colitis (UC). The aim of this study was to comp…
Tacrolimus vs. anti-tumour necrosis factor agents for moderately to severely ac…
PMID: 26762838
Year: 2016
Relationship Type:
Treatment
Score: 6.3
BACKGROUND: There have been no comparative studies of tacrolimus vs. anti-tumour necrosis factor (anti-TNF) agents to determine which treatment is sa…
Successful use of infliximab and tacrolimus combination therapy in a patient wi…
PMID: 26754306
Year: 2016
Relationship Type:
Treatment
Score: 6.3
OBJECTIVE: To report of a case successful use of infliximab (IFX) and tacrolimus (TAC) in a patient with ulcerative colitis (UC). CASE SUMMARY: A 22-…
Efficacy and Safety of Tacrolimus Therapy for Active Ulcerative Colitis; A Syst…
PMID: 26645641
Year: 2016
Relationship Type:
Treatment
Score: 6.3
BACKGROUND: Approximately 25% of patients with ulcerative colitis [UC] experience a severe flare requiring steroid therapy to avoid colectomy. We per…
Long-term Outcomes in Steroid-refractory Ulcerative Colitis Treated with Tacrol…
PMID: 26419459
Year: 2016
Relationship Type:
Treatment
Score: 6.3
BACKGROUND AND AIMS: Tacrolimus is recommended for the treatment of steroid-refractory ulcerative colitis (UC). Concomitantly started purine analogue…
[Efficiency of tacrolimus therapy for perianal Crohn's disease]
PMID: 26281201
Year: 2015
Relationship Type:
Treatment
Score: 6.3
AIM: To determine the efficacy of 0.1% tacrolimus ointment in patients with perianal Crohn's disease (CD). SUBJECTS AND METHODS: This prospective ran…
Successful use of infliximab and tacrolimus in a patient with Crohn's disease
PMID: 25997551
Year: 2015
Relationship Type:
Treatment
Score: 6.3
OBJECTIVE: To report a case of successful use of infliximab (IFX) and tacrolimus (TAC) in a patient with Crohn's disease (CD). CASE SUMMARY: A 42-yea…