| Drug ID: | Drug112 |
|---|---|
| Drug Name: | Tofacitinib |
| CID: | 9926791 |
| DrugBank ID: | DB08895 |
| Modality: | Small Molecule |
| Groups: | approved |
| US Approved: | YES |
| Other Approved: | YES |
| Identifier: | NCT00787202, , NCT03281304, , NCT01458574, , NCT01470612, , NCT06625450, , NCT04424303, , NCT05112263, , NCT06095128, , NCT05728008, , NCT05431283, , NCT05313620, , NCT04925973, , NCT06780683, , NCT06274996, , NCT05782907, , NCT06095596, , NCT03653026, , NCT02819635, , NCT03345836, , NCT03006 |
| Molecular Formula: | C16H20N6O |
| Molecular Weight: | 312.37 g/mol |
| Isomeric SMILES: | C[C@@H]1CCN(C[C@@H]1N(C)C2=NC=NC3=C2C=CN3)C(=O)CC#N |
| Synonyms: | Tofacitinib; 477600-75-2; 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile; Cp-690 free base; tofacitinibum; UNII-87LA6FU830; CHEBI:71200; 87LA6FU830; CP-690550 FREE BASE; CP-690,550 FREE BASE |
| Phase 0: | 6 |
| Phase 1: | 84 |
| Phase 2: | 131 |
| Phase 3: | 80 |
| Phase 4: | 39 |
| Description: | Tofacitinib is an inhibitor of Janus kinases, a group of intracellular enzymes involved in signaling pathways that affect hematopoiesis and immune cell function. It is approved by the FDA for treatment of moderate to severe rheumatoid arthritis that responds inadequately to methotrexate or in those who are intolerant to methotrexate. Besides rheumatoid arthritis, tofacitinib has also been studied in clinical trials for the prevention of organ transplant rejection, and the treatment of psoriasis and ulcerative colitis. Known adverse effects include nausea and headache as well as more serious immunologic and hematological adverse effects. Tofacitinib is marketed under the brand name Xeljanz. |
Molecular Structure
Knowledge Graph
| dtID | CID | Compound Name | Gene ID | Gene Name | Species | PubMed IDs | Action |
|---|---|---|---|---|---|---|---|
| dt948 | 9926791 | Tofacitinib | 2048 | EPHB2 | Homo sapiens (human) | Inhibitor | |
| dt949 | 9926791 | Tofacitinib | 6777 | STAT5B | Homo sapiens (human) | None | |
| dt950 | 9926791 | Tofacitinib | 3716 | JAK1 | Homo sapiens (human) | Inhibitor | |
| dt951 | 9926791 | Tofacitinib | 3718 | JAK3 | Homo sapiens (human) | None | |
| dt952 | 9926791 | Tofacitinib | 29110 | TBK1 | Homo sapiens (human) | 25540906 | None |
| dt953 | 9926791 | Tofacitinib | 3717 | JAK2 | Homo sapiens (human) | 24417533 | Inhibition |
| dt954 | 9926791 | Tofacitinib | 3718 | JAK3 | Homo sapiens (human) | Inhibition | |
| dt955 | 9926791 | Tofacitinib | 3718 | JAK3 | Homo sapiens (human) | 24417533 | Inhibition |
| dt956 | 9926791 | Tofacitinib | 3718 | JAK3 | Homo sapiens (human) | 27572962 | Inhibition |
| dt957 | 9926791 | Tofacitinib | 3716 | JAK1 | Homo sapiens (human) | 24417533 | Inhibition |
- 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 | |
|---|---|---|---|---|---|---|---|
| NCT05431283 | Real-world Effectiveness of Tofacitinib on Ulcerative Colitis Associated Spondyloarthropathy | NULL | UNKNOWN | Italian Group for the study of Inflammatory Bowel Disease (IG-IBD) | Ulcerative Colitis|Spondyloarthropathy | DRUG: Tofacitinib | Details |
| NCT05313620 | Effect of Tofacitinib on Coagulation and Platelet Function, and Its Role in Thromboembolic Events | PHASE4 | RECRUITING | Fundación de Investigación Biomédica - Hospital Universitario de La Princesa | Ulcerative Colitis|Thromboembolism | DRUG: Tofacitinib|DRUG: Infliximab Adalimumab y G… | Details |
| NCT07138898 | Immunosuppressant Management in Rheumatology Patients Undergoing Elective Total Shoulder Arthroplasty | PHASE2 | NOT_YET_RECRUITING | NYU Langone Health | Rheumatic Disease | DRUG: Methotrexate|DRUG: Sulfasalazine|DRUG: Hydr… | Details |
| NCT05186623 | Prediction Model for Response to Biologics and Small Molecular Agent for UC | NULL | RECRUITING | Asan Medical Center | Ulcerative Colitis | DRUG: Vedolizumab, Ustekinumab, or Tofacitinib | Details |
| NCT05112263 | Tofacitinib Versus Cyclosporine for Steroid Refractory Acute Severe Ulcerative Colitis | NA | NOT_YET_RECRUITING | Post Graduate Institute of Medical Education and Research, Chandigarh | Ulcerative Colitis | DRUG: Tofacitinib|DRUG: Cyclosporine | Details |
| NCT05104723 | Safety and Efficacy of Tofacitinib for Chronic Granulomatous Disease With Inflammatory Complications | PHASE1|PHASE2 | ENROLLING_BY_INVITATION | National Institute of Allergy and Infectious Diseases (NIAID) | Chronic Granulomatous Disease|Inflammatory Gastro… | DRUG: XELJANZ (tofacitinib) | Details |
| NCT05082428 | This Study is to Describe and Evaluate Patients in Finland Treated With Tofacitinib for the Treatment of Ulcerative Colitis Using Real World Data. | NULL | COMPLETED | Pfizer | Ulcerative Colitis | None | Details |
| NCT05069259 | Generate Real World Data On Tofacitinib Induction Therapy and Changes In Clinical and Patient Reported Outcomes. | NULL | TERMINATED | Pfizer | Ulcerative Colitis | OTHER: Stool sample collection | Details |
| NCT04925973 | Tofacitinib for Hospitalized Acute Severe Ulcerative Colitis Management | PHASE2 | ACTIVE_NOT_RECRUITING | McMaster University | Ulcerative Colitis Acute | DRUG: Tofacitinib 10 MG [Xeljanz] | Details |
| NCT04743518 | Impact of Anti-TNF, Vedolizumab and Tofacitinib on Aortic Stiffness, Carotid Intima-media Thickness and Cardiovascular Risk of Patients With Ulcerative Colitis | PHASE4 | RECRUITING | Centre Hospitalier Universitaire, Amiens | Ulcerative Colitis | OTHER: Aortic pulse wave velocity|OTHER: carotid … | Details |
| NCT04624230 | Evaluation of Oral Tofacitinib in Children Aged 2 to 17 Years Old Suffering From Moderate to Severe Ulcerative Colitis | PHASE3 | ACTIVE_NOT_RECRUITING | Pfizer | Ulcerative Colitis | DRUG: tofacitinib | Details |
| NCT04424303 | Tofacitinib in Adult Patients With Moderate to Severe Ulcerative Colitis | NULL | COMPLETED | Pfizer | Ulcerative Colitis | DRUG: Tofacitinib | Details |
| NCT04338204 | Observational Study To Assess The Effectiveness and Treatment Adherence Of Tofacitinib of Ulcerative Colitis In Clinical Practice In Sweden | NULL | RECRUITING | Pfizer | Ulcerative Colitis | DRUG: tofacitinib | Details |
| NCT04032756 | Tofacitinib Registry of Patients With Ulcerative Colitis in Germany | NULL | TERMINATED | Ced Service GmbH | Colitis, Ulcerative|Biologics|Tofacitiniib|Chroni… | None | Details |
| NCT03885713 | Identification of Predictive Biomarkers for Response to Biologic Therapies and Tofacitinib in Inflammatory Bowel Disease | PHASE4 | COMPLETED | Fundación de Investigación Biomédica - Hospital Universitario de La Princesa | Inflammatory Bowel Diseases|Crohn Disease|Ulcerat… | BIOLOGICAL: Infliximab or adalimumab or golimumab… | Details |
| NCT03772145 | Tofacitinib Response in Ulcerative Colitis - a Real World Prospective Multi-center Study | NULL | TERMINATED | University of North Carolina, Chapel Hill | Ulcerative Colitis | None | Details |
| NCT03663400 | Identify Predictors That Distinguish Between Tofacitinib Responders and Non-responders Based on Genotype and Cellular and Molecular Profiles From Pinch Biopsies, Blood and Stool Samples | NULL | COMPLETED | NYU Langone Health | Ulcerative Colitis | DIAGNOSTIC_TEST: GWAS analysis by Illumina BeadCh… | Details |
| NCT03591770 | Shingrix Vaccine in Patients With Moderate to Severe Ulcerative Colitis on Tofacitinib | PHASE4 | TERMINATED | Boston Medical Center | Inflammatory Bowel Diseases | BIOLOGICAL: SHINGRIX | Details |
| NCT03281304 | A Study of Tofacitinib in Patients With Ulcerative Colitis in Stable Remission | PHASE4 | TERMINATED | Pfizer | Ulcerative Colitis | DRUG: CP-690,500 5 mg|DRUG: CP-690,550 10 mg | Details |
| NCT03103412 | TD-3504 SAD in Healthy Subjects and Subjects With Ulcerative Colitis (UC) | PHASE1 | COMPLETED | Theravance Biopharma | Active Mild Ulcerative Colitis, Active Moderate U… | DRUG: TD-3504|DRUG: 15N2-tofacitinib|DRUG: Placebo | Details |
| Disease ID | Disease Name | Definition | Category | Related Drugs | Mechanism | |
|---|---|---|---|---|---|---|
| No data available | ||||||
| Strategy ID | Therapeutic Strategy | Synonyms | Related Drugs | Mechanism | |
|---|---|---|---|---|---|
| S07 | Blockade of cytokine | Cytokine signalling | apremilast; roflumilast; filgotinib; tofacitinib; ABT494; ABT-874; ustekinumab; isankizumab; LY-2525623; AMG139; MEDI2079; guselkumab | Various T-cell subsets, their differentiation pathways and … | Details |
Upfront tofacitinib in patients with biological-naïve ulcerative colitis - An I…
PMID: 37726491
Year: 2024
Relationship Type:
Treatment
Score: 6.5
OBJECTIVES: Tofacitinib is a Janus Kinase inhibitor used for treating moderate to severe ulcerative colitis (UC), mainly after the failure of biologi…
Experience with Tofacitinib in Patients with Ulcerative Colitis: Data from a Un…
PMID: 37639057
Year: 2023
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Tofacitinib is an oral small molecule Janus kinase inhibitor for the treatment of ulcerative colitis (UC). AIMS: To evaluate real-world d…
Outcomes of Tofacitinib Use in an Irish Pediatric Cohort
PMID: 37600624
Year: 2023
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Pediatric ulcerative colitis (UC) is typically more extensive and severe at diagnosis compared with adult disease. Tofacitinib, a Janus k…
Outcomes out to 12 months after sequential use of high-dose tofacitinib followi…
PMID: 37599224
Year: 2023
Relationship Type:
Treatment
Score: 6.5
Acute severe colitis (ASUC) remains a significant cause of morbidity in up to 25% of patients with ulcerative colitis during their disease course. We…
Presence of risk factors associated with colectomy among patients with ulcerati…
PMID: 37560161
Year: 2023
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Tofacitinib is an oral small molecule Janus kinase inhibitor for the treatment of ulcerative colitis (UC). OBJECTIVE: To assess colectomy…
Real-Life Efficacy of Tofacitinib in Various Situations in Ulcerative Colitis: …
PMID: 37542737
Year: 2024
Relationship Type:
Treatment
Score: 6.5
BACKGROUND AND AIMS: Tofacitinib (TFB) appears to be effective in the treatment of ulcerative colitis (UC); however, available real-world studies are…
Tofacitinib-induced eosinophilia
PMID: 37539549
Year: 2023
Relationship Type:
Treatment
Score: 6.5
Tofacitinib is an oral small molecule JAK inhibitor approved for the treatment of moderate to severe ulcerative colitis (UC). Its efficacy and safety…
Modeling of Treatment Outcomes with Tofacitinib Maintenance Therapy in Patients…
PMID: 37525075
Year: 2023
Relationship Type:
Treatment
Score: 6.5
INTRODUCTION: Tofacitinib is an oral small molecule Janus kinase inhibitor for the treatment of ulcerative colitis (UC). This post hoc analysis asses…
P004 Steroid-Free Remission in Patients With Ulcerative Colitis Receiving Tofac…
PMID: 37461925
Year: 2021
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Tofacitinib is a selective immunosuppressant, the first representative of the inhibitors of the janus kinase family, which has high selec…
Major Adverse Cardiovascular Events by Baseline Cardiovascular Risk in Patients…
PMID: 37402275
Year: 2023
Relationship Type:
Treatment
Score: 6.5
BACKGROUND AND AIMS: Patients with inflammatory bowel disease have increased risk of atherosclerotic cardiovascular [CV] disease [ASCVD]. Tofacitinib…
Manifestation of acute appendicitis as known but paradox visceral side effect o…
PMID: 37393666
Year: 2023
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: The etiopathogenesis of accompanying inflammatory phenomena and consequences of immunomodulation constitute a challenging and innovative …
Use of tofacitinib as first or second-line therapy is associated with better ou…
PMID: 37358928
Year: 2023
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Data regarding the real-world (RW) use of tofacitinib (TOF) in patients with ulcerative colitis (UC) are limited. We aimed to investigate…
Comparing Patient-Reported Outcomes Among Anti-TNF Experienced Patients With Ul…
PMID: 37350775
Year: 2023
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Primary and secondary nonresponse to anti-tumor necrosis factor (TNF) therapy is common in patients with ulcerative colitis (UC), yet lim…
The current role of Tofacitinib in acute severe ulcerative colitis in adult pat…
PMID: 37316363
Year: 2023
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Despite rescue therapy, acute severe ulcerative colitis (ASUC) is associated with a high risk of colectomy, while treatment options remai…
Impact of biological agents and tofacitinib for moderate-to-severe ulcerative c…
PMID: 37313882
Year: 2021
Relationship Type:
Treatment
Score: 6.5
INTRODUCTION: In the past few years, several options have been proposed as alternative and more effective therapeutic drugs for moderate-to-severe ul…
Delayed and limited administration of the JAKinib tofacitinib mitigates chronic…
PMID: 37275854
Year: 2023
Relationship Type:
Treatment
Score: 6.5
In inflammatory bowel disease, dysregulated T cells express pro-inflammatory cytokines. Using a chronic azoxymethane (AOM)/dextran sulfate sodium (DS…
Real-World Experience With Tofacitinib Dose De-Escalation in Patients With Mode…
PMID: 37187323
Year: 2023
Relationship Type:
Treatment
Score: 6.5
BACKGROUND & AIMS: Tofacitinib is associated with sustained steroid-free remission in patients with ulcerative colitis (UC), with the lowest effectiv…
Tofacitinib to Treat Severe Acute Refractory Colitis in a Teenager: Case Report…
PMID: 37168636
Year: 2022
Relationship Type:
Treatment
Score: 6.5
Acute severe colitis (ASC) may occur within 3 months of ulcerative colitis diagnosis in 9%-15% of children and the rate of colectomy is up to 40%-50%…
Comparative Efficacy of Infliximab Versus Tofacitinib for Inducing Remission in…
PMID: 37119375
Year: 2023
Relationship Type:
Treatment
Score: 6.5
OBJECTIVE: In the absence of head-to-head clinical trials, indirect comparative studies are needed to help position therapies in ulcerative colitis (…
Tofacitinib experience in patients with enteropathic arthritis
PMID: 37009645
Year: 2023
Relationship Type:
Treatment
Score: 6.5
Background/aim: The JAK-STAT pathway is involved in the pathogenesis of both the inflammatory bowel disease (IBD) and spondyloarthropathy group of di…