| 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 Treatment Safety in Moderate to Severe Ulcerative Colitis: Comparis…
PMID: 33324993
Year: 2021
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Tofacitinib is an oral, small molecule Janus kinase inhibitor for the treatment of ulcerative colitis (UC). We aimed to estimate the over…
Tofacitinib for the Treatment of Ulcerative Colitis: Analysis of Infection Rate…
PMID: 33245746
Year: 2021
Relationship Type:
Treatment
Score: 6.5
BACKGROUND AND AIMS: Tofacitinib is an oral, small molecule JAK inhibitor for the treatment of ulcerative colitis. We report integrated analyses of i…
Efficacy and Safety of Extended Induction With Tofacitinib for the Treatment of…
PMID: 33127596
Year: 2022
Relationship Type:
Treatment
Score: 6.5
BACKGROUND & AIMS: Tofacitinib is an oral, small molecule Janus kinase inhibitor for the treatment of ulcerative colitis (UC). The efficacy and safet…
Cost-effectiveness analysis of infliximab, adalimumab, golimumab, vedolizumab a…
PMID: 33097619
Year: 2020
Relationship Type:
Treatment
Score: 6.5
OBJECTIVE: Despite the biological drugs, the treatment of moderate to severe ulcerative colitis is still a challenge, particularly in resource-limite…
Maintenance of Remission With Tofacitinib Therapy in Patients With Ulcerative C…
PMID: 33039585
Year: 2022
Relationship Type:
Treatment
Score: 6.5
BACKGROUND & AIMS: Tofacitinib is an oral, small molecule Janus kinase inhibitor for the treatment of ulcerative colitis (UC). The efficacy and safet…
Cost-effectiveness of tofacitinib for the treatment of moderate to severe activ…
PMID: 32976189
Year: 2021
Relationship Type:
Treatment
Score: 6.5
OBJECTIVE: To evaluate the cost-effectiveness of tofacitinib versus other treatment options currently available for the management of adult patients …
Tofacitinib in Ulcerative Colitis: Real-world Evidence From the ENEIDA Registry
PMID: 32969471
Year: 2021
Relationship Type:
Adverse Effect
Score: 6.5
AIM: To evaluate the effectiveness and safety of tofacitinib in ulcerative colitis [UC] in real life. METHODS: Patients from the prospectively mainta…
Cost-Effectiveness of 5-Aminosalicylate Therapy in Combination With Biologics o…
PMID: 32947317
Year: 2021
Relationship Type:
Treatment
Score: 6.5
INTRODUCTION: Medications are major cost drivers in the treatment of patients with inflammatory bowel disease. Recent analyses suggest that there is …
Pharmacology and safety of tofacitinib in ulcerative colitis
PMID: 32829958
Year: 2021
Relationship Type:
Treatment
Score: 6.5
The use of Janus kinase (JAK) inhibitors is a new approach in the therapy of inflammatory diseases with immune base. Tofacitinib is one of these inhi…
Characterization of Creatine Kinase Levels in Tofacitinib-Treated Patients with…
PMID: 32816215
Year: 2021
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Tofacitinib is an oral, small-molecule JAK inhibitor for the treatment of ulcerative colitis (UC). Creatine kinase (CK) levels and CK-rel…
The JAK1/3 inhibitor tofacitinib suppresses T cell homing and activation in chr…
PMID: 32808031
Year: 2021
Relationship Type:
Treatment
Score: 6.5
BACKGROUND & AIMS: The molecular mechanism of action of the Janus kinase (JAK) inhibitor tofacitinib is poorly understood. METHODS: Here, we analysed…
Tofacitinib in Patients with Ulcerative Colitis: Inflammatory Bowel Disease Que…
PMID: 32794567
Year: 2021
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Tofacitinib is an oral, small molecule Janus kinase inhibitor for the treatment of ulcerative colitis (UC). We examined the effect of tof…
Tofacitinib, an Oral Janus Kinase Inhibitor: Analysis of Malignancy (Excluding …
PMID: 32766762
Year: 2021
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Tofacitinib is an oral, small molecule Janus kinase inhibitor for the treatment of ulcerative colitis (UC). Here, we performed an integra…
Tofacitinib in Treatment-Refractory Moderate to Severe Ulcerative Colitis: Real…
PMID: 32664204
Year: 2020
Relationship Type:
Treatment
Score: 6.5
(1) Background: Tofacitinib is approved in Europe for the treatment of adults with moderately to severely active ulcerative colitis since 2018. Real-…
Two cases in which tofacitinib effectively treated both ulcerative colitis and …
PMID: 32592149
Year: 2020
Relationship Type:
Treatment
Score: 6.5
A 40-year-old woman (case 1) visited the hospital complaining of diarrhea and was diagnosed with ulcerative colitis (UC). She was administered 5-amin…
Safety of New Biologics (Vedolizumab and Ustekinumab) and Small Molecules (Tofa…
PMID: 32562207
Year: 2020
Relationship Type:
Treatment
Score: 6.5
Two new biological drugs (vedolizumab and ustekinumab) and one small molecule (tofacitinib) have been recently approved for the treatment of inflamma…
Is tofacitinib a game-changing drug for ulcerative colitis?
PMID: 32552501
Year: 2020
Relationship Type:
Treatment
Score: 6.5
The increasing knowledge on ulcerative colitis' pathophysiology has contributed to the expansion of the therapeutic arsenal for this condition. Howev…
Comparison of the effects of tofacitinib and adalimumab on transcolonoscopic ph…
PMID: 32285809
Year: 2020
Relationship Type:
Treatment
Score: 6.5
OBJECTIVE: The aim: To investigate the transcolonoscopic pH-metry and calprotectin in patients with ulcerative colitis. PATIENTS AND METHODS: Materia…
Tofacitinib for ulcerative colitis: results of the prospective Dutch Initiative…
PMID: 32237087
Year: 2020
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Tofacitinib is a Janus kinase inhibitor approved for the treatment of ulcerative colitis (UC). AIM: To evaluate effectiveness, safety and…
Tofacitinib for Rescue Therapy in Acute Severe Ulcerative Colitis: A Real-world…
PMID: 32020189
Year: 2020
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Acute severe ulcerative colitis is a high stakes event with significant numbers still requiring emergent colectomy, representing a need t…