| 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 |
Histologic Features of Tacrolimus-induced Colonic Injury
PMID: 34138798
Year: 2022
Relationship Type:
Treatment
Score: 6.5
Tacrolimus is a common immunosuppressant used in solid organ transplant recipients. Although most patients develop diarrheal symptoms, data regarding…
The impact of cytochrome P450 3A genetic polymorphisms on tacrolimus pharmacoki…
PMID: 33886687
Year: 2021
Relationship Type:
Treatment
Score: 6.5
Tacrolimus (Tac) is an effective remission inducer of refractory ulcerative colitis (UC). Gene polymorphisms result in interindividual variability in…
Combination of Vedolizumab With Tacrolimus Is More Efficient Than Vedolizumab A…
PMID: 33847343
Year: 2021
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Vedolizumab is a widely used and safe therapy in inflammatory bowel disease, particularly in ulcerative colitis (UC), making it a promisi…
3D printed tacrolimus suppositories for the treatment of ulcerative colitis
PMID: 33613734
Year: 2021
Relationship Type:
Treatment
Score: 6.5
Ulcerative colitis is a global health problem, affecting millions of individuals worldwide. As an inflammatory condition localised in the large intes…
3D Printed Tacrolimus Rectal Formulations Ameliorate Colitis in an Experimental…
PMID: 33276641
Year: 2020
Relationship Type:
Treatment
Score: 6.5
The aim of this study was to fabricate novel self-supporting tacrolimus suppositories using semisolid extrusion 3-dimensional printing (3DP) and to i…
Efficacy of infliximab, cyclosporine and tacrolimus on ulcerative colitis: A me…
PMID: 33126341
Year: 2020
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Positioning infliximab (IFX), cyclosporine and tacrolimus (TAC) for treating ulcerative colitis (UC) is in great debate. METHODS: A liter…
Comparative efficacy of antitumor necrosis factor agents and tacrolimus in naïv…
PMID: 32719413
Year: 2020
Relationship Type:
Treatment
Score: 6.5
While retrospective studies have compared the efficacy of anti-tumour necrosis factor (TNF) agents and tacrolimus (TAC) in ulcerative colitis (UC), i…
Relationship between mucosal healing by tacrolimus and relapse of refractory ul…
PMID: 32590945
Year: 2020
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Tacrolimus (TAC) is a powerful remission-inducing drug for refractory ulcerative colitis (UC). However, it is unclear whether mucosal hea…
CYP3A5 Genotype as a Potential Pharmacodynamic Biomarker for Tacrolimus Therapy…
PMID: 32570960
Year: 2020
Relationship Type:
Treatment
Score: 6.5
Tacrolimus has been used to induce remission in patients with steroid-refractory ulcerative colitis. It poses a problem of large individual differenc…
Effectiveness and Nephrotoxicity of Long-Term Tacrolimus Administration in Pati…
PMID: 32517388
Year: 2020
Relationship Type:
Adverse Effect
Score: 6.5
BACKGROUND: Tacrolimus (TAC) is used for the management of ulcerative colitis (UC). However, there are few reports on the effectiveness of its long-t…
Colon-Targeted Therapy of Tacrolimus (FK506) in the Treatment of Experimentally…
PMID: 31940656
Year: 2020
Relationship Type:
Treatment
Score: 6.5
BACKGROUND/AIMS: Inflammatory bowel disease is a chronic or remitting/relapsing intestinal inflammation, which comprises Crohn's disease and ulcerati…
Azathioprine Is Useful for Maintaining Long-term Remission Induced by Tacrolimu…
PMID: 31118391
Year: 2019
Relationship Type:
Treatment
Score: 6.5
Objective The need for and efficacy of immunomodulators for maintaining remission after tacrolimus therapy have not been sufficiently defined. This s…
Appropriate Timing of Discontinuation of Tacrolimus Therapy for Refractory Ulce…
PMID: 31065933
Year: 2019
Relationship Type:
Treatment
Score: 6.5
BACKGROUND AND OBJECTIVES: Tacrolimus is very effective at inducing remission in patients with refractory ulcerative colitis. However, the optimal ti…
Therapeutic Efficacy and Adverse Events of Tacrolimus in Patients with Crohn's …
PMID: 30982208
Year: 2019
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Only a few randomized controlled trials (RCTs) and some uncontrolled trials have reported the efficacy and adverse events (AEs) of tacrol…
Tacrolimus Therapy in Steroid-Refractory Ulcerative Colitis: A Review
PMID: 30980713
Year: 2020
Relationship Type:
Treatment
Score: 6.5
Inflammatory bowel diseases are known for a chronic inflammatory process of the gastrointestinal tract and include Crohn's disease and ulcerative col…
Pretreatment neutrophil-to-lymphocyte ratio predicts clinical relapse of ulcera…
PMID: 30845259
Year: 2019
Relationship Type:
Treatment
Score: 6.5
OBJECTIVES: Although tacrolimus is useful as an induction therapy in patients with ulcerative colitis (UC), information regarding the long-term outco…
Tacrolimus Suppositories in Therapy-Resistant Ulcerative Proctitis
PMID: 30820433
Year: 2019
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Ulcerative proctitis may often be managed with topical salicylates or steroids alone, but in some patients, symptoms are persistent and s…
Rapid attainment of target trough concentrations of tacrolimus for early improv…
PMID: 30604428
Year: 2019
Relationship Type:
Treatment
Score: 6.5
WHAT IS KNOWN AND OBJECTIVE: The target trough concentration of tacrolimus for ulcerative colitis is recommended to be 10-15 ng/mL in the initial two…
Long-lasting immunosuppressive effects of tacrolimus-loaded micelle NK61060 in …
PMID: 30277135
Year: 2018
Relationship Type:
Pharmacology
Score: 6.3
AIM: Tacrolimus (TAC) is an important drug for inflammatory diseases. However, TAC has several limitations, such as variable trough concentrations am…
Pooled analysis of the comparative efficacy between tacrolimus and infliximab f…
PMID: 30095612
Year: 2018
Relationship Type:
Treatment
Score: 6.3
BACKGROUND: Acute moderate-to-severe steroid-refractory ulcerative colitis (UC) has a poor prognosis and requires optimal rescue therapy. A pooled an…