| 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 | |
|---|---|---|---|---|---|---|---|
| NCT05431283 | Real-world Effectiveness of Tofacitinib on Ulcerative Colitis Associated Spondyloarthropathy | NULL | UNKNOWN | Italian Group for the study of Inflammatory Bowel Disease (IG-IBD) | Ulcerative Colitis|Spondyloarthropathy | DRUG: Tofacitinib | 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 |
| NCT07138898 | Immunosuppressant Management in Rheumatology Patients Undergoing Elective Total Shoulder Arthroplasty | PHASE2 | NOT_YET_RECRUITING | NYU Langone Health | Rheumatic Disease | DRUG: Methotrexate|DRUG: Sulfasalazine|DRUG: Hydr… | Details |
| NCT05186623 | Prediction Model for Response to Biologics and Small Molecular Agent for UC | NULL | RECRUITING | Asan Medical Center | Ulcerative Colitis | DRUG: Vedolizumab, Ustekinumab, or Tofacitinib | Details |
| NCT05112263 | Tofacitinib Versus Cyclosporine for Steroid Refractory Acute Severe Ulcerative Colitis | NA | NOT_YET_RECRUITING | Post Graduate Institute of Medical Education and Research, Chandigarh | Ulcerative Colitis | DRUG: Tofacitinib|DRUG: Cyclosporine | 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 |
| NCT05082428 | This Study is to Describe and Evaluate Patients in Finland Treated With Tofacitinib for the Treatment of Ulcerative Colitis Using Real World Data. | NULL | COMPLETED | Pfizer | Ulcerative Colitis | None | Details |
| NCT05069259 | Generate Real World Data On Tofacitinib Induction Therapy and Changes In Clinical and Patient Reported Outcomes. | NULL | TERMINATED | Pfizer | Ulcerative Colitis | OTHER: Stool sample collection | Details |
| NCT04925973 | Tofacitinib for Hospitalized Acute Severe Ulcerative Colitis Management | PHASE2 | ACTIVE_NOT_RECRUITING | McMaster University | Ulcerative Colitis Acute | DRUG: Tofacitinib 10 MG [Xeljanz] | Details |
| NCT04743518 | Impact of Anti-TNF, Vedolizumab and Tofacitinib on Aortic Stiffness, Carotid Intima-media Thickness and Cardiovascular Risk of Patients With Ulcerative Colitis | PHASE4 | RECRUITING | Centre Hospitalier Universitaire, Amiens | Ulcerative Colitis | OTHER: Aortic pulse wave velocity|OTHER: carotid … | Details |
| NCT04624230 | Evaluation of Oral Tofacitinib in Children Aged 2 to 17 Years Old Suffering From Moderate to Severe Ulcerative Colitis | PHASE3 | ACTIVE_NOT_RECRUITING | Pfizer | Ulcerative Colitis | DRUG: tofacitinib | Details |
| NCT04424303 | Tofacitinib in Adult Patients With Moderate to Severe Ulcerative Colitis | NULL | COMPLETED | Pfizer | Ulcerative Colitis | DRUG: Tofacitinib | Details |
| NCT04338204 | Observational Study To Assess The Effectiveness and Treatment Adherence Of Tofacitinib of Ulcerative Colitis In Clinical Practice In Sweden | NULL | RECRUITING | Pfizer | Ulcerative Colitis | DRUG: tofacitinib | Details |
| NCT04032756 | Tofacitinib Registry of Patients With Ulcerative Colitis in Germany | NULL | TERMINATED | Ced Service GmbH | Colitis, Ulcerative|Biologics|Tofacitiniib|Chroni… | None | Details |
| NCT03885713 | Identification of Predictive Biomarkers for Response to Biologic Therapies and Tofacitinib in Inflammatory Bowel Disease | PHASE4 | COMPLETED | Fundación de Investigación Biomédica - Hospital Universitario de La Princesa | Inflammatory Bowel Diseases|Crohn Disease|Ulcerat… | BIOLOGICAL: Infliximab or adalimumab or golimumab… | Details |
| NCT03772145 | Tofacitinib Response in Ulcerative Colitis - a Real World Prospective Multi-center Study | NULL | TERMINATED | University of North Carolina, Chapel Hill | Ulcerative Colitis | None | 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 | NULL | COMPLETED | NYU Langone Health | Ulcerative Colitis | DIAGNOSTIC_TEST: GWAS analysis by Illumina BeadCh… | Details |
| NCT03591770 | Shingrix Vaccine in Patients With Moderate to Severe Ulcerative Colitis on Tofacitinib | PHASE4 | TERMINATED | Boston Medical Center | Inflammatory Bowel Diseases | BIOLOGICAL: SHINGRIX | Details |
| NCT03281304 | A Study of Tofacitinib in Patients With Ulcerative Colitis in Stable Remission | PHASE4 | TERMINATED | Pfizer | Ulcerative Colitis | DRUG: CP-690,500 5 mg|DRUG: CP-690,550 10 mg | 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 |
| 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 Versus Vedolizumab Among Bio-naive Patients With Ulcerative Colitis…
PMID: 39659234
Year: 2025
Relationship Type:
Treatment
Score: 6.5
BACKGROUND AND AIMS: Over the last decade, treatment options for moderate-to-severe ulcerative colitis (UC) have expanded. However, comparative studi…
Dual action tofacitinib-loaded PLGA nanoparticles alleviate colitis in an IBD m…
PMID: 39527394
Year: 2025
Relationship Type:
Treatment
Score: 6.5
Inflammatory bowel disease (IBD) affects over 7 million people worldwide and significant side effects are associated with current therapies such as t…
The JAK inhibitor, Tofacitinib, Corrects the Overexpression of CEACAM6 and Limi…
PMID: 39399045
Year: 2024
Relationship Type:
Association
Score: 6.5
BACKGROUND AND AIMS: A cohort of patients with inflammatory bowel disease (IBD) exhibit expansion of the gut pathobiont, adherent-invasive E. coli (A…
Tofacitinib in Pediatric Ulcerative Colitis: A Retrospective Multicenter Experi…
PMID: 38828483
Year: 2025
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Tofacitinib has recently been approved for treatment of moderate-to-severe ulcerative colitis (UC) in adults, yet pediatric data are limi…
Effect of tofacitinib on the phenotype and activity of Caco‑2 cells in a model …
PMID: 38476894
Year: 2024
Relationship Type:
Treatment
Score: 6.5
Reports have indicated that autoimmune bowel disorders affect an increasing number of people on every continent; therefore, it is important to better…
Changes in HLA-B27 Transgenic Rat Fecal Microbiota Following Tofacitinib Treatm…
PMID: 38396840
Year: 2024
Relationship Type:
Treatment
Score: 6.5
The therapeutic management of Crohn's disease (CD), a chronic relapsing-remitting inflammatory bowel disease (IBD), is highly challenging. Surgical r…
Tofacitinib use in ulcerative colitis: An expert consensus for day-to-day clini…
PMID: 38347433
Year: 2024
Relationship Type:
Treatment
Score: 6.5
Rising number of inflammatory bowel disease (IBD) cases in developing countries necessitate clear guidance for clinicians for the appropriate use of …
Normal Infant Immunologic Assessment and Uneventful Live Rotavirus Vaccination …
PMID: 38317692
Year: 2024
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Janus kinase (JAK) inhibitors are effective for the treatment of inflammatory bowel disease (IBD). However, this class of medications is …
Tofacitinib in Pregnancy: Assessing Pregnancy and Infant Outcomes, Cord Blood, …
PMID: 38309493
Year: 2025
Relationship Type:
Treatment
Score: 6.5
Janus kinase (JAK) inhibitors are effective anti-inflammatory agents for treatment of ulcerative colitis (UC).(1) According to drug regulatory agenci…
Rates of Adverse Events in Patients With Ulcerative Colitis Undergoing Colectom…
PMID: 38305302
Year: 2024
Relationship Type:
Treatment
Score: 6.5
INTRODUCTION: Patients with ulcerative colitis (UC) receiving immunosuppressive drugs are at substantial risk of colectomy. We aimed to assess the ri…
Tofacitinib real-world experience in ulcerative colitis in Finland (FinTofUC): …
PMID: 38156792
Year: 2024
Relationship Type:
Treatment
Score: 6.5
OBJECTIVES: The aim was to define the effectiveness of tofacitinib and to characterize the patient population receiving tofacitinib in a real-world c…
Tofacitinib Affects M1-like and M2-like Polarization and Tissue Factor Expressi…
PMID: 38142236
Year: 2024
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Tofacitinib, as inhibitor of Janus kinases (JAK), interrupts the transmission of numerous pro-inflammatory cytokines involved in the path…
Tofacitinib in Acute Severe Ulcerative Colitis (TACOS): A Randomized Controlled…
PMID: 38131615
Year: 2024
Relationship Type:
Treatment
Score: 6.5
INTRODUCTION: Intravenous corticosteroids are the mainstay of treatment of patients hospitalized with acute severe ulcerative colitis (ASUC). However…
Histological healing induced by tofacitinib in ulcerative colitis: A multicentr…
PMID: 38065698
Year: 2024
Relationship Type:
Association
Score: 6.5
BACKGROUND: While the efficacy of tofacitinib to induce and maintain clinical and endoscopic remission is well established in ulcerative colitis (UC)…
Early recapture of response with tofacitinib 10 mg twice daily in patients with…
PMID: 37953548
Year: 2024
Relationship Type:
Treatment
Score: 6.5
BACKGROUND AND AIM: Tofacitinib is an oral Janus kinase inhibitor for the treatment of ulcerative colitis. These post hoc analyses evaluated early im…
Antibody Responses to Influenza Vaccination are Diminished in Patients With Inf…
PMID: 37941436
Year: 2024
Relationship Type:
Treatment
Score: 6.5
BACKGROUND AND AIMS: We sought to determine whether six commonly used immunosuppressive regimens were associated with lower antibody responses after …
Tofacitinib in Steroid-Refractory Acute Severe Ulcerative Colitis: A Retrospect…
PMID: 37854768
Year: 2023
Relationship Type:
Treatment
Score: 6.5
INTRODUCTION: Steroid-refractory acute severe ulcerative colitis (ASUC) patients are at the highest risk of colectomy. Among the available options, c…
Tofacitinib in the treatment of moderate to severe ulcerative colitis in Colomb…
PMID: 37820832
Year: 2024
Relationship Type:
Treatment
Score: 6.5
INTRODUCTION: There are no studies on efficacy of tofacitinib for moderate-severe ulcerative colitis (UC) in pediatric patients in Latin America. The…
Colombian experience with the use of tofacitinib in severe acute ulcerative col…
PMID: 37806342
Year: 2024
Relationship Type:
Treatment
Score: 6.5
INTRODUCTION: Tofacitinib is indicated in patients with moderate to severe ulcerative colitis (UC); however, given its rapid onset of action, it may …
Safety and effectiveness of tofacitinib in ulcerative colitis: Data from TOFA-U…
PMID: 37741749
Year: 2024
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Real-world evidence is needed to determine the value of tofacitinib (TOFA) for the treatment of ulcerative colitis (UC). AIM: To assess t…