| 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-Induced Modulation of Intestinal Adaptive and Innate Immunity and F…
PMID: 34624526
Year: 2022
Relationship Type:
Treatment
Score: 6.5
OBJECTIVE: By interfering with multiple cytokines, human Janus kinase inhibitors (JAKis) are of growing importance in the treatment of malignant and …
Agreement between local and central reading of endoscopic disease activity in u…
PMID: 34614208
Year: 2021
Relationship Type:
Association
Score: 6.5
BACKGROUND: Endoscopy is routine in trials of ulcerative colitis therapies. AIM: To investigate agreement between central and local Mayo endoscopic s…
Effectiveness and Safety of Tofacitinib for Ulcerative Colitis: Systematic Revi…
PMID: 34516458
Year: 2022
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: The objective of our systematic review and meta-analysis was to evaluate the effectiveness and safety of tofacitinib in the treatment of …
Real-World Efficacy and Safety Monitoring for Predicting Continuation of Tofaci…
PMID: 34460029
Year: 2022
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Although the clinical efficacy of tofacitinib in patients with ulcerative colitis (UC) has been assessed in the OCTAVE trial, there is a …
Success of Cyclosporin and Tofacitinib Combination Therapy in a Patient With Se…
PMID: 34398196
Year: 2021
Relationship Type:
Treatment
Score: 6.5
At present, the conventional therapies for acute severe ulcerative colitis (ASUC) mainly include corticosteroids, cyclosporin, and biological agents.…
Safety and Efficacy of Tofacitinib in Combination With Biologic Therapy for Ref…
PMID: 34347103
Year: 2022
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: The majority of patients with Crohn's disease (CD) will not achieve endoscopic remission on current therapy. Addition of tofacitinib to b…
Efficacy and Safety of Tofacitinib for Treatment of Moderate to Severe Active U…
PMID: 34196200
Year: 2021
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Tofacitinib, a selective inhibitor of JAK/STAT pathway, has recently become available in our region. Here, we examined the safety and eff…
Sequential Use of High-Dose Tofacitinib After Infliximab Salvage Therapy in Acu…
PMID: 34159363
Year: 2022
Relationship Type:
Treatment
Score: 6.5
BACKGROUND AND AIMS: Preliminary data regarding the effectiveness of tofacitinib in acute severe ulcerative colitis [ASUC] have been presented in two…
Tofacitinib as salvage therapy for 55 patients hospitalised with refractory sev…
PMID: 34151448
Year: 2021
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Up to 25% of patients with ulcerative colitis (UC) will require hospitalization for severe flare. In patients hospitalised for severe fla…
Tofacitinib for Biologic-Experienced Hospitalized Patients With Acute Severe Ul…
PMID: 34048936
Year: 2021
Relationship Type:
Treatment
Score: 6.5
BACKGROUND & AIMS: Despite rescue therapy, more than 30% of patients with acute severe ulcerative colitis (ASUC) require colectomy. Tofacitinib is a …
Adverse events of special interest in clinical trials of rheumatoid arthritis, …
PMID: 34045358
Year: 2021
Relationship Type:
Adverse Effect
Score: 6.5
OBJECTIVES: To analyse adverse events (AEs) of special interest across tofacitinib clinical programmes in rheumatoid arthritis (RA), psoriatic arthri…
Perioperative safety of tofacitinib in surgical ulcerative colitis patients
PMID: 33942470
Year: 2021
Relationship Type:
Association
Score: 6.5
AIM: The literature regarding monoclonal antibodies and increased postoperative complications in inflammatory bowel disease remains controversial. Th…
Efficacy and Safety of Tofacitinib Re-treatment for Ulcerative Colitis After Tr…
PMID: 33884415
Year: 2021
Relationship Type:
Treatment
Score: 6.5
BACKGROUND AND AIMS: Tofacitinib is an oral, small molecule Janus kinase inhibitor for the treatment of ulcerative colitis. Here, we evaluate the eff…
Tofacitinib for the treatment of refractory pyoderma gangrenosum
PMID: 33864685
Year: 2021
Relationship Type:
Treatment
Score: 6.5
Pyoderma gangrenosum (PG) is a rare, debilitating, inflammatory skin disease associated with a variety of systemic diseases. Because of its rarity, P…
Tofacitinib for the Treatment of Ulcerative Colitis: Analysis of Nonmelanoma Sk…
PMID: 33742652
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). We present integrated analyse…
Efficacy and Safety of Tofacitinib in Ulcerative Colitis Based on Prior Tumor N…
PMID: 33684552
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). We summarize the effic…
Guideline review: Tofacitinib for adults with moderately to severely active ulc…
PMID: 33613945
Year: 2020
Relationship Type:
Treatment
Score: 6.5
Tofacitinib is an oral, Janus kinase (JAK) molecule, which selectively inhibits Janus-associated tyrosine kinases JAK1 and JAK3. It has already shown…
Cost-effectiveness of tofacitinib compared with infliximab, adalimumab, golimum…
PMID: 33502905
Year: 2021
Relationship Type:
Treatment
Score: 6.5
OBJECTIVES: Tofacitinib is an oral, small molecule Janus kinase (JAK) inhibitor for the treatment of ulcerative colitis (UC). This study assessed the…
A patient with ulcerative colitis treated with a combination of vedolizumab and…
PMID: 33495165
Year: 2021
Relationship Type:
Treatment
Score: 6.5
Ulcerative colitis (UC) is an inflammatory bowel disease of autoimmune origin with an estimated prevalence in Spain of 0.39%. Current treatments for …
Real-world clinical and endoscopic outcomes after one year tofacitinib treatmen…
PMID: 33405424
Year: 2021
Relationship Type:
Treatment
Score: 6.5
OBJECTIVE: Tofacitinib, an oral Janus kinase inhibitor, is approved for the treatment of moderate to severe ulcerative colitis (UC). We evaluated cli…