| 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 |
Tofacitinib
PMID: 21171673
Year: 2010
Relationship Type:
Treatment
Score: 7.1
Tofacitinib (CP-690,550; CP-690550; CP690550), an orally active immunosuppressant, is being developed by Pfizer for the treatment of rheumatoid arthr…
Prospective observational study of tofacitinib in ulcerative colitis - analysis…
PMID: 40535533
Year: 2025
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Tofacitinib is a Janus kinase inhibitor for the treatment of ulcerative colitis (UC). Prospective real-world data are scarce. OBJECTIVES:…
Real-life effectiveness and safety of tofacitinib and vedolizumab as 2nd-line f…
PMID: 40335332
Year: 2025
Relationship Type:
Treatment
Score: 6.5
BACKGROUND AND AIMS: Drug positioning in ulcerative colitis (UC) patients refractory to anti-tumor necrosis factor (TNF) is still debated. In a natio…
Differential effects of tofacitinib on macrophage activation contribute to lack…
PMID: 40320713
Year: 2025
Relationship Type:
Treatment
Score: 6.5
BACKGROUND AND AIMS: Tofacitinib, a Janus kinase inhibitor, is approved for the treatment of moderate-to-severe ulcerative colitis. Nonetheless, 40-6…
Post-marketing surveillance of tofacitinib in patients with ulcerative colitis …
PMID: 40259041
Year: 2025
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: We present the final analysis of a tofacitinib post-marketing surveillance (PMS) study in Japanese patients with ulcerative colitis (UC).…
Drug tissue concentration and STAT3 modulation as determinants of tofacitinib r…
PMID: 40243193
Year: 2025
Relationship Type:
Treatment
Score: 6.5
INTRODUCTION: Inflammatory bowel disease management has advanced with therapies like Janus kinase inhibitors (JAKi). Despite their promise, JAKi phar…
Postoperative Outcomes in Tofacitinib-Treated Patients With Acute Severe Ulcera…
PMID: 40239733
Year: 2025
Relationship Type:
Treatment
Score: 6.5
BACKGROUND AND AIMS: Up to 30% of patients with acute severe ulcerative colitis (ASUC) will require urgent colectomy despite initiation of intravenou…
Inflammatory bowel disease therapeutics: a bibliometric analysis of tofacitinib…
PMID: 40235538
Year: 2025
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Ulcerative colitis (UC) is a chronic inflammatory bowel disease affecting millions worldwide. Tofacitinib, an inhibitor of Janus kinase (…
Restoration of colonic barrier function by tofacitinib in experimental colitis:…
PMID: 40159830
Year: 2025
Relationship Type:
Treatment
Score: 6.5
BACKGROUND/AIMS: Inflammatory bowel disease can be triggered by disturbances in intestinal mucosal integrity, leading to bacterial transmigration. Th…
Real-World Experience With Tofacitinib in Steroid-Dependent Patients With Moder…
PMID: 40130137
Year: 2025
Relationship Type:
Treatment
Score: 6.5
INTRODUCTION: Patients with moderate-to-severe ulcerative colitis (UC) who are steroid-dependent despite being on immunomodulators pose significant c…
Effect of tofacitinib exposure in utero and during breastfeeding on the immune …
PMID: 40127036
Year: 2025
Relationship Type:
Treatment
Score: 6.5
BACKGROUND AND AIMS: Janus kinase (JAK) inhibitors, such as tofacitinib, are potent anti-inflammatory agents used in the treatment of ulcerative coli…
Tofacitinib for ulcerative colitis in Brazil: a multicenter observational study…
PMID: 40102788
Year: 2025
Relationship Type:
Treatment
Score: 6.5
AIM: To assess the real-life, long-term effectiveness and safety of tofacitinib in a large cohort of patients with refractory or difficult-to-treat u…
Upadacitinib Results in Endoscopic Remission in Patients With Inflammatory Bowe…
PMID: 40063408
Year: 2025
Relationship Type:
Treatment
Score: 6.5
GOALS: Assess the safety and effectiveness of upadacitinib in patients with prior tofacitinib failure. BACKGROUND: Patients with severe, refractory C…
Potential predictors of efficacy outcomes following tofacitinib dose reduction …
PMID: 40028509
Year: 2025
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Tofacitinib is an oral Janus kinase inhibitor for the treatment of ulcerative colitis (UC). OBJECTIVES: To investigate potential predicto…
Efficacy and safety of tofacitinib for the treatment of moderate-to-severe ulce…
PMID: 39976073
Year: 2025
Relationship Type:
Treatment
Score: 6.5
BACKGROUND AND AIMS: Tofacitinib has been approved for the treatment of patients with moderate-to-severe ulcerative colitis independently of prior th…
Activated type 17 helper T cells affect tofacitinib treatment outcomes
PMID: 39971758
Year: 2025
Relationship Type:
Treatment
Score: 6.5
The incidence of ulcerative colitis (UC) is on the rise also in Japan. Simultaneously, therapeutic options, including biologics and Janus kinase (JAK…
Tofacitinib for the treatment of chronic pouchitis: A pilot study
PMID: 39895228
Year: 2025
Relationship Type:
Treatment
Score: 6.5
BACKGROUND & AIMS: Up to 15% of ulcerative colitis (UC) patients with an ileo-anal pouch will develop chronic or antibiotic refractory pouchitis. We …
Tofacitinib and budesonide treatment affect stemness and chemokine release in I…
PMID: 39885201
Year: 2025
Relationship Type:
Treatment
Score: 6.5
Restoration of the intestinal epithelial barrier is crucial for achieving mucosal healing, the therapeutic goal for inflammatory bowel disease (IBD).…
Continuous Treatment with Tofacitinib but Not Filgotinib Is Effective in Non-Re…
PMID: 39797304
Year: 2025
Relationship Type:
Treatment
Score: 6.5
Background: Few studies have compared the efficacy and safety of Janus kinase (JAK) inhibitors in patients with ulcerative colitis (UC). We compared …
Tofacitinib Mitigates the Increased SARS-CoV-2 Infection Susceptibility Caused …
PMID: 39756517
Year: 2025
Relationship Type:
Treatment
Score: 6.5
BACKGROUND & AIMS: Coronavirus disease (COVID-19), caused by severe acquired respiratory syndrome-Coronavirus-2 (SARS-CoV-2), triggered a global pand…