| 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 |
Effects of oral tacrolimus as a rapid induction therapy in ulcerative colitis
PMID: 25684955
Year: 2015
Relationship Type:
Treatment
Score: 6.3
AIM: To determine the efficacy and safety of rapid induction therapy with oral tacrolimus without a meal in steroid-refractory ulcerative colitis (UC…
Tacrolimus for remission induction in ulcerative colitis: Mayo endoscopic subsc…
PMID: 25682993
Year: 2015
Relationship Type:
Treatment
Score: 6.3
BACKGROUND: Tacrolimus has shown efficacy in patients with ulcerative colitis. AIMS: To evaluate the efficacy of tacrolimus as remission induction th…
Severe diffuse duodenitis successfully treated with intravenous tacrolimus afte…
PMID: 25366006
Year: 2014
Relationship Type:
Treatment
Score: 6.3
We encountered a rare case of severe diffuse duodenitis associated with ulcerative colitis (UC). A 23-year-old man underwent total proctocolectomy wi…
Oral tacrolimus for the treatment of refractory inflammatory bowel disease in t…
PMID: 23615528
Year: 2013
Relationship Type:
Treatment
Score: 6.1
BACKGROUND: Patients with inflammatory bowel disease who are refractory to standard therapies frequently require surgery. The long-term efficacy of t…
[A case of tacrolimus plus intensive LCAP therapy combination for refractory ul…
PMID: 23558127
Year: 2013
Relationship Type:
Treatment
Score: 6.1
A 30-year-old woman was referred to our hospital with recurrent refractory ulcerative colitis. She also suffered from avascular necrosis of the left …
Tacrolimus salvage in anti-tumor necrosis factor antibody treatment-refractory …
PMID: 23518805
Year: 2013
Relationship Type:
Treatment
Score: 6.1
BACKGROUND: Several small retrospective studies have reported encouraging response rates in patients with Crohn's disease (CD) treated with tacrolimu…
The efficacy of oral tacrolimus in patients with moderate/severe ulcerative col…
PMID: 23291669
Year: 2013
Relationship Type:
Treatment
Score: 6.1
OBJECTIVE: The calcineurin inhibitor tacrolimus has been shown to be safe and effective as salvage therapy for steroid-refractory ulcerative colitis …
Short-term efficacy of tacrolimus in steroid-refractory ulcerative colitis - ex…
PMID: 23121200
Year: 2013
Relationship Type:
Treatment
Score: 6.1
BACKGROUND: Steroid-refractory ulcerative colitis (UC) remains a challenging condition warranting surgery upon failure of pharmacological treatment. …
Combination therapy of tacrolimus and infliximab reduces inflammatory response …
PMID: 22167049
Year: 2012
Relationship Type:
Treatment
Score: 6.1
BACKGROUND: Intestinal transplantation initiates a functionally relevant inflammatory response by activation of resident macrophages within the muscu…
Systematic review: the role of tacrolimus in the management of Crohn's disease
PMID: 21999607
Year: 2011
Relationship Type:
Treatment
Score: 6.1
BACKGROUND Several published studies have evaluated the efficacy of tacrolimus in the management of Crohn's disease with variable conclusions. AIM …
Double-blind, placebo-controlled trial of oral tacrolimus (FK506) in the manage…
PMID: 21887732
Year: 2012
Relationship Type:
Treatment
Score: 6.1
BACKGROUND: We report a multicenter study of oral tacrolimus (FK506) therapy in steroid-refractory ulcerative colitis (UC). METHODS: In a placebo-con…
ABCB1 single-nucleotide polymorphisms determine tacrolimus response in patients…
PMID: 21289623
Year: 2011
Relationship Type:
Treatment
Score: 6.1
Tacrolimus (Tac) is effective in the treatment of steroid-refractory ulcerative colitis (UC); however, nonresponse and unpredictable side effects are…
Two cases of fatal Pneumocystis jirovecii pneumonia as a complication of tacrol…
PMID: 21122569
Year: 2010
Relationship Type:
Treatment
Score: 6.1
Here we report 2 cases of fatal Pneumocystis jirovecii pneumonia in patients with severe ulcerative colitis receiving combination immunosuppression i…
Topical tacrolimus for parastomal pyoderma gangrenosum: a report of two cases
PMID: 20855912
Year: 2010
Relationship Type:
Treatment
Score: 6.1
Pyoderma gangrenosum (PG) is an idiopathic, ulcerative, inflammatory dermatologic condition that occurs in patients with systemic diseases such as i…
Immunosuppressive effects of tacrolimus on macrophages ameliorate experimental …
PMID: 20848491
Year: 2010
Relationship Type:
Association
Score: 6.1
BACKGROUND: Tacrolimus is a novel immunomodulator for inflammatory bowel diseases. Immunosuppressive effects of tacrolimus on T cells are well known;…
Outcomes and adverse events in children and young adults undergoing tacrolimus …
PMID: 20722055
Year: 2011
Relationship Type:
Treatment
Score: 6.1
BACKGROUND: Children with severe corticosteroid-resistant ulcerative colitis either need to undergo surgery or be treated with more intensive immunos…
Efficacy and safety of infliximab as rescue therapy for ulcerative colitis refr…
PMID: 20546441
Year: 2010
Relationship Type:
Treatment
Score: 6.1
BACKGROUND AND AIM: Little is known about the efficacy and safety of infliximab for ulcerative colitis refractory to tacrolimus. The aim of this stud…
Infliximab as rescue medication for patients with severe ulcerative/indetermina…
PMID: 20175769
Year: 2010
Relationship Type:
Treatment
Score: 6.1
BACKGROUND: The calcineurin inhibitor tacrolimus and the anti-TNF-antibody infliximab are established options in steroid-refractory ulcerative coliti…
Tacrolimus (FK506): Safety and Applications in Reconstructive Surgery
PMID: 19363638
Year: 2010
Relationship Type:
Treatment
Score: 6.1
Tacrolimus (FK506) is a macrolide immunosuppressive drug that is approved for the prevention of allograft rejection. It is a standard component of im…