| 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 | |
|---|---|---|---|---|---|---|---|
| NCT04624230 | Evaluation of Oral Tofacitinib in Children Aged 2 to 17 Years Old Suffering From Moderate to Severe Ulcerative Colitis | PHASE3 | RECRUITING | Pfizer | Ulcerative Colitis | DRUG: tofacitinib | Details |
| NCT01465763 | A Study Evaluating The Efficacy And Safety Of CP-690,550 In Patients With Moderate To Severe Ulcerative Colitis | PHASE3 | COMPLETED | Pfizer | Ulcerative Colitis | DRUG: tofacitinib|DRUG: Placebo | Details |
| NCT04032756 | Tofacitinib Registry of Patients With Ulcerative Colitis in Germany | None | TERMINATED | Ced Service GmbH | Colitis, Ulcerative|Biologics|Tofacitiniib|Chroni… | None | Details |
| NCT01458951 | A Study To Evaluate Both The Efficacy and Safety Profile of CP-690,550 In Patients With Moderately to Severely Active Ulcerative Colitis | PHASE3 | COMPLETED | Pfizer | Ulcerative Colitis | DRUG: tofacitinib|DRUG: Placebo | Details |
| NCT05112263 | Tofacitinib Versus Cyclosporine for Steroid Refractory Acute Severe Ulcerative Colitis | None | NOT_YET_RECRUITING | Post Graduate Institute of Medical Education and Research, Chandigarh | Ulcerative Colitis | DRUG: Tofacitinib|DRUG: Cyclosporine | Details |
| NCT06469424 | An Active Surveillance, Post-Authorization Study to Characterize the Safety of Tofacitinib in Patients With Moderately to Severely Active Ulcerative Colitis in the Real-World Setting Using Data From the United Registries for Clinical Assessment and Research (UR-CARE) in the European Union (EU) | None | RECRUITING | Grupo Espanol de Trabajo en Enfermedad de Crohn y Colitis Ulcerosa | Ulcerative Colitis | None | Details |
| NCT06095128 | A Study of Vedolizumab With Tofacitinib in Adults With Ulcerative Colitis (UC) | PHASE4 | RECRUITING | Takeda | Ulcerative Colitis | DRUG: Vedolizumab|DRUG: Tofacitinib | Details |
| NCT05728008 | Retrospective Observational Comparison Study Between Ustekinumab and Tofacitinib as Third Line Therapy in a Multicenter Cohort of Patients With Refractory Ulcerative Colitis. | None | COMPLETED | IRCCS San Raffaele | Ulcerative Colitis | DRUG: Ustekinumab|DRUG: Tofacitinib | Details |
| NCT04743518 | Impact of Anti-TNF, Vedolizumab and Tofacitinib on Aortic Stiffness, Carotid Intima-media Thickness and Cardiovascular Risk of Patients With Ulcerative Colitis | None | UNKNOWN | Centre Hospitalier Universitaire, Amiens | Ulcerative Colitis | OTHER: Aortic pulse wave velocity|OTHER: carotid … | 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 |
| NCT05431283 | Real-world Effectiveness of Tofacitinib on Ulcerative Colitis Associated Spondyloarthropathy | None | UNKNOWN | Italian Group for the study of Inflammatory Bowel Disease (IG-IBD) | Ulcerative Colitis|Spondyloarthropathy | DRUG: Tofacitinib | 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 |
| NCT05069259 | Generate Real World Data On Tofacitinib Induction Therapy and Changes In Clinical and Patient Reported Outcomes. | None | TERMINATED | Pfizer | Ulcerative Colitis | OTHER: Stool sample collection | 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 | None | COMPLETED | NYU Langone Health | Ulcerative Colitis | DIAGNOSTIC_TEST: GWAS analysis by Illumina BeadCh… | 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 |
| CTRI/2024/01/061649 | Prevalence and impact of sarcopenia and frailty in inflammatory bowel disease, and the effect of multi-modal interventions on sarcopenia and clinical outcomes in patients with inflammatory bowel disease - NIL | PHASE3 | Not Recruiting | All India Institute of Medical Sciences | Health Condition 1: K509- Crohns disease, unspeci… | Intervention1: High protein anti-inflammatory die… | Details |
| CTRI/2023/10/058514 | Evaluation of effectiveness and safety of oral tofacitinib in patients with Parthenium dermatitis: A prospective interventional open label study - NIL | Not Available | Not Recruiting | AIIMS, New Delhi | Health Condition 1: L237- Allergic contact dermat… | Intervention1: Oral Tofacitinib: Tofacitinib is a… | Details |
| ISRCTN96296121 | Defining microbial predictors of responsiveness to biologic therapies in Crohn disease and ulcerative colitis | Not Available | Recruiting | Newcastle upon Tyne Hospitals NHS Foundation Trust | Crohn disease and ulcerative colitis Digestive S… | Current interventions as of 19/12/2024: This is… | Details |
| ISRCTN13495664 | SARS-CoV2 Vaccination immunogenicity in Immunosuppressed inflammatory bowel disease Patients | Not Available | Not Recruiting | Imperial College London | Immune responses to SARS-CoV-2 vaccination in imm… | 600 IBD patients will be recruited stratified acc… | 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 |
| 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…