| 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 |
Comparison of the safety and efficacy of fingolimod and tofacitinib in the zebr…
PMID: 36343746
Year: 2022
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Oral targeted small molecules, including sphingosine 1 phosphate receptor (S1PR) modulators and tyrosine kinase inhibitors (TKIs), seem t…
Assessment of Safety and Efficacy of Tofacitinib, Stratified by Age, in Patient…
PMID: 36342120
Year: 2023
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: In patients with ulcerative colitis (UC), risks of infection and malignancies increase with age. Tofacitinib is an oral, small molecule J…
Long-Term Improvement in the Patient-Reported Outcomes of Rectal Bleeding, Stoo…
PMID: 36336750
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). The tofacitinib OCTAVE clinica…
Health-Related Quality of Life Outcomes With Tofacitinib Treatment in Patients …
PMID: 36242764
Year: 2023
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Tofacitinib is an oral small molecule Janus kinase inhibitor for the treatment of ulcerative colitis. We report health-related quality of…
Endo-histologic Normalization Is Achievable with Tofacitinib and Is Associated …
PMID: 36242686
Year: 2023
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Recent real-world effectiveness studies investigating tofacitinib have been encouraging. Questions remain regarding the long-term effecti…
Clinical Case of Tofacitinib Therapy in Autoimmune Alopecia in Patient with Ulc…
PMID: 36185344
Year: 2022
Relationship Type:
Treatment
Score: 6.5
This article presents the clinical case of a patient with a long history of ulcerative colitis. Seven years after the onset of the disease, other aut…
Tofacitinib for the Treatment of Ulcerative Colitis: An Integrated Summary of u…
PMID: 36124702
Year: 2023
Relationship Type:
Treatment
Score: 6.5
BACKGROUND AND AIMS: Tofacitinib is an oral small molecule Janus kinase [JAK] inhibitor for the treatment of ulcerative colitis. We report an integra…
Tofacitinib Salvage Therapy for Children Hospitalized for Corticosteroid- and B…
PMID: 36122389
Year: 2022
Relationship Type:
Treatment
Score: 6.5
OBJECTIVES: Colectomy rates following acute severe ulcerative colitis have plateaued around 20% despite intravenous corticosteroid and intensified an…
Review article: guide to tofacitinib dosing in patients with ulcerative colitis
PMID: 35993338
Year: 2022
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Tofacitinib is an oral small molecule Janus kinase inhibitor for the treatment of ulcerative colitis (UC). The induction dose is 10 mg tw…
Positioning of tofacitinib in treatment of ulcerative colitis: a global perspec…
PMID: 35875997
Year: 2022
Relationship Type:
Treatment
Score: 6.5
INTRODUCTION: Tofacitinib has emerged as a useful drug for the treatment of ulcerative colitis (UC). AREAS COVERED: There is an unmet need for cost-e…
Effects of Dextran Sulfate Sodium-Induced Ulcerative Colitis on the Disposition…
PMID: 35811297
Year: 2022
Relationship Type:
Treatment
Score: 6.5
Tofacitinib, a Janus kinase 1 and 3 inhibitor, is mainly metabolized by CYP3A1/2 and CYP2C11 in the liver. The drug has been approved for the chronic…
Clostridium difficile Infection in Patients with Ulcerative Colitis Treated wit…
PMID: 35792493
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). Patients with inflammatory bo…
Safety and efficacy of long-term tofacitinib treatment in East Asian patients w…
PMID: 35734858
Year: 2022
Relationship Type:
Treatment
Score: 6.5
BACKGROUND AND AIM: Tofacitinib is an oral small molecule Janus kinase inhibitor for the treatment of ulcerative colitis (UC). We present safety and …
Tofacitinib Response in Ulcerative Colitis (TOUR): Early Response After Initiat…
PMID: 35700276
Year: 2023
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Tofacitinib is an oral, small-molecule JAK inhibitor for the treatment of ulcerative colitis (UC). Using a novel electronic reporting too…
Tofacitinib Downregulates TNF and Poly(I:C)-Dependent MHC-II Expression in the …
PMID: 35655783
Year: 2022
Relationship Type:
Treatment
Score: 6.5
Major Histocompatibility Complex (MHC)-I and -II genes are upregulated in intestinal epithelial cells (IECs) during active inflammatory bowel disease…
Long-term Risk of Herpes Zoster Infection in Patients With Ulcerative Colitis R…
PMID: 35648151
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). We report herpes zoster (HZ) …
Superior Effectiveness of Tofacitinib Compared to Vedolizumab in Anti-TNF-exper…
PMID: 35644343
Year: 2023
Relationship Type:
Treatment
Score: 6.5
BACKGROUND & AIMS: Clinicians face difficulty in when and in what order to position biologics and Janus kinase inhibitors in patients with anti-tumor…
Corticosteroid-free efficacy and safety outcomes in patients receiving tofaciti…
PMID: 35574426
Year: 2022
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 report steroid-free …
Bridging Efficacy of Tofacitinib Immediate-Release to Extended-Release Formulat…
PMID: 35560874
Year: 2022
Relationship Type:
Treatment
Score: 6.5
Tofacitinib is an oral, small molecule Janus kinase inhibitor for the treatment of ulcerative colitis (UC). We report a model-informed drug developme…
Longitudinal monitoring of STAT3 phosphorylation and histologic outcome of tofa…
PMID: 35484689
Year: 2022
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Tofacitinib is the first in class, pan-JAK inhibitor approved for ulcerative colitis (UC). Clinical efficacy has been shown, but long-ter…