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

2D Molecular Structure

Knowledge Graph

dtIDCIDCompound NameGene IDGene NameSpeciesPubMed IDsAction
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 IDTitlePhaseStatusSponsorIndicationsInterventions
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 IDDisease NameDefinitionCategoryRelated DrugsMechanism
No data available

Strategy IDTherapeutic StrategySynonymsRelated DrugsMechanism
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 for the treatment of ulcerative colitis

PMID: 27177233
Year: 2016
Relationship Type: Treatment Score: 6.3

INTRODUCTION: Management of patients with active ulcerative colitis (UC), one of the most frequent inflammatory bowel diseases in human beings, is ma…

Tofacitinib in ulcerative colitis

PMID: 27140405
Year: 2016
Relationship Type: Treatment Score: 6.3

Cytokines orchestrate immune and inflammatory responses involved in the pathogenesis of ulcerative colitis (UC). Protein kinases are essential for si…

Tofacitinib

PMID: 31643187
Year: 2012
Relationship Type: Treatment Score: 6.1

Tofacitinib is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis, psoriatic arthritis …

Tofacitinib for the treatment of rheumatoid arthritis

PMID: 22607178
Year: 2012
Relationship Type: Treatment Score: 6.1

Rheumatoid arthritis (RA) is a chronic inflammatory disease that affects approximately 1% of the worldwide population. It primarily targets the synov…

A phase 2 study of tofacitinib, an oral Janus kinase inhibitor, in patients wit…

PMID: 24480677
Year: Unknown
Relationship Type: Adverse Effect Score: 6.0

BACKGROUND & AIMS: Tofacitinib, an orally administered Janus kinase inhibitor, blocks signaling through gamma-chain-containing cytokines (interleukin…

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