Tofacitinib

Summary

Tofacitinib (CHEMBL221959) is an approved small-molecule EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor (ATC L04AF01) targeting PKN1, JAK1, and JAK2; indicated across 35 conditions including rheumatoid arthritis and psoriatic arthritis.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: L04AF01
• Targets: 5 (PKN1, JAK1, JAK2…)
• Indications: 35 conditions
• Clinical trials: 204
• Chemistry: 312.37 Da · C16H20N6O

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL221959
Name	Tofacitinib
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	9926791
ChEBI	CHEBI:71200
ATC	L04AF01
Molecular formula	C16H20N6O
Molecular weight	312.37
InChIKey	UJLAWZDWDVHWOW-YPMHNXCESA-N

SMILES: C[C@@H]1CCN(C[C@@H]1N(C)C2=NC=NC3=C2C=CN3)C(=O)CC#N

IUPAC name: 3-[(3R,4R)-4-methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile

ChEBI definition: A pyrrolopyrimidine that is pyrrolo[2,3-d]pyrimidine substituted at position 4 by an N-methyl,N-(1-cyanoacetyl-4-methylpiperidin-3-yl)amino moiety. Used as its citrate salt to treat moderately to severely active rheumatoid arthritis.

Pharmacological roles (ChEBI): EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor, antirheumatic drug.

Also known as: CP 690550, CP- 690 550, CP-690, Cp-690 free base, CP-690,550, CP-690,550 FREE BASE, CP-690550, CP-690550 FREE BASE, CP690,550, CP690550, Tofacitinib, TOFACITINIB

Parent form; salt/anhydrous children: CHEMBL2103743

Patent coverage: 4,136 distinct patent families (10,408 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 9,748 (94%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
PKN1	protein kinase N1	Inhibition	6.91	1.5%	Q16512
JAK1	Janus kinase 1	Inhibition	7.82	2.8%	P23458
JAK2	Janus kinase 2	Inhibition	7.11	0.7%	O60674
JAK3	Janus kinase 3	Inhibition	7.26	0.6%	P52333
TYK2	tyrosine kinase 2	Inhibition	6.31	0.8%	P29597

Broader ChEMBL bioactivity targets: 57 (assay-derived). Sample: Leucine-rich repeat serine/threonine-protein kinase 2, Rhodopsin kinase GRK7, Tyrosine-protein kinase JAK2, Transient receptor potential cation channel subfamily M member 6, Tyrosine-protein kinase JAK2, Tyrosine-protein kinase Fyn, Tyrosine-protein kinase ABL1, Serine/threonine-protein kinase PknB, Proto-oncogene tyrosine-protein kinase receptor Ret, Tyrosine-protein kinase JAK3, Aurora kinase B, Janus Kinase (JAK), Calcium/calmodulin-dependent protein kinase type 1, Ribosomal protein S6 kinase alpha-1, Tyrosine-protein kinase Lck, Vascular endothelial growth factor receptor 2, Calcium/calmodulin-dependent protein kinase type II subunit delta, Tyrosine-protein kinase JAK1, 3’,5’-cyclic-AMP phosphodiesterase 4D, Tyrosine-protein kinase JAK1.

Bioactivity

ChEMBL activities: 449 potent at pChembl ≥ 5 of 452 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
JAK3	9.8	Kd	0.16	nM	CHEMBL_ACT_7567638
JAK3	9.7	Ki	0.2	nM	CHEMBL_ACT_24861794
JAK3	9.62	Ki	0.24	nM	CHEMBL_ACT_12062097
JAK3	9.62	IC50	0.24	nM	CHEMBL_ACT_18737105
JAK3	9.62	Ki	0.24	nM	CHEMBL_ACT_26239383
JAK3	9.62	IC50	0.24	nM	CHEMBL_ACT_27736817
JAK3	9.54	IC50	0.29	nM	CHEMBL_ACT_18298420
JAK3	9.54	IC50	0.29	nM	CHEMBL_ACT_26230166
JAK3	9.47	IC50	0.34	nM	CHEMBL_ACT_18148544
JAK3	9.46	IC50	0.35	nM	CHEMBL_ACT_16515197
JAK3	9.4	Ki	0.4	nM	CHEMBL_ACT_12063038
JAK3	9.4	Ki	0.4	nM	CHEMBL_ACT_13317434
JAK3	9.4	Ki	0.4	nM	CHEMBL_ACT_13330000
TYK2	9.4	IC50	0.4	nM	CHEMBL_ACT_25701609
JAK3	9.4	IC50	0.4	nM	CHEMBL_ACT_25851482
JAK1	9.3	IC50	0.5	nM	CHEMBL_ACT_18298400
JAK2	9.3	IC50	0.5	nM	CHEMBL_ACT_19489470
JAK1	9.3	IC50	0.5	nM	CHEMBL_ACT_26230156
JAK2	9.24	Kd	0.58	nM	CHEMBL_ACT_7567830
JAK2	9.22	IC50	0.6	nM	CHEMBL_ACT_15112130
JAK3	9.22	IC50	0.6	nM	CHEMBL_ACT_8009762
JAK1	9.19	Ki	0.64	nM	CHEMBL_ACT_22391387
JAK1	9.17	Ki	0.68	nM	CHEMBL_ACT_12062095
JAK1	9.17	Ki	0.68	nM	CHEMBL_ACT_26239381
JAK1	9.15	Ki	0.7	nM	CHEMBL_ACT_12062103
JAK2	9.15	Ki	0.7	nM	CHEMBL_ACT_12063027
JAK2	9.15	Ki	0.7	nM	CHEMBL_ACT_13317435
JAK1	9.15	Ki	0.7	nM	CHEMBL_ACT_13317436
JAK2	9.15	Ki	0.7	nM	CHEMBL_ACT_13331561
JAK1	9.15	Ki	0.7	nM	CHEMBL_ACT_13331595
JAK3	9.15	IC50	0.7	nM	CHEMBL_ACT_19489439
JAK1	9.15	Ki	0.7	nM	CHEMBL_ACT_24861790
JAK1	9.15	IC50	0.7	nM	CHEMBL_ACT_25851476
JAK2	9.15	IC50	0.7	nM	CHEMBL_ACT_25851479
JAK3	9.15	Kd	0.7	nM	CHEMBL_ACT_2595780
JAK1	9.1	IC50	0.8	nM	CHEMBL_ACT_15112083
JAK3	9.1	IC50	0.8	nM	CHEMBL_ACT_15648411
JAK3	9.1	IC50	0.8	nM	CHEMBL_ACT_24692009
JAK3	9.1	IC50	0.8	nM	CHEMBL_ACT_25039696
JAK3	9.05	IC50	0.9	nM	CHEMBL_ACT_22471543
JAK3	9.01	IC50	0.98	nM	CHEMBL_ACT_22809475
JAK2	9	Ki	0.99	nM	CHEMBL_ACT_12062096
JAK3	9	IC50	1	nM	CHEMBL_ACT_15082443
JAK3	9	IC50	1	nM	CHEMBL_ACT_18789042
JAK2	9	IC50	1	nM	CHEMBL_ACT_18991827
JAK3	9	IC50	1	nM	CHEMBL_ACT_24788512
JAK2	9	Ki	1	nM	CHEMBL_ACT_24861792
JAK3	9	IC50	1	nM	CHEMBL_ACT_25650367
JAK3	9	IC50	0.99	nM	CHEMBL_ACT_25675040
JAK3	9	IC50	1	nM	CHEMBL_ACT_2595776
JAK2	9	Ki	0.99	nM	CHEMBL_ACT_26239382
JAK3	9	IC50	1	nM	CHEMBL_ACT_29122445
JAK3	9	Ki	1	nM	CHEMBL_ACT_3447701
JAK3	9	IC50	1	nM	CHEMBL_ACT_5109056
JAK2	8.96	IC50	1.09	nM	CHEMBL_ACT_18737128
JAK3	8.96	IC50	1.1	nM	CHEMBL_ACT_18991866
JAK3	8.96	IC50	1.1	nM	CHEMBL_ACT_20714727
JAK2	8.96	IC50	1.09	nM	CHEMBL_ACT_27736814
JAK3	8.92	IC50	1.2	nM	CHEMBL_ACT_16796987
JAK2	8.92	IC50	1.2	nM	CHEMBL_ACT_20714961
JAK1	8.9	IC50	1.26	nM	CHEMBL_ACT_25675094
JAK1	8.89	IC50	1.3	nM	CHEMBL_ACT_16515209
JAK1	8.89	IC50	1.3	nM	CHEMBL_ACT_18148494
JAK1	8.89	IC50	1.3	nM	CHEMBL_ACT_19264112
JAK1	8.89	IC50	1.3	nM	CHEMBL_ACT_22471623
JAK3	8.85	IC50	1.4	nM	CHEMBL_ACT_13901971
JAK2	8.85	IC50	1.4	nM	CHEMBL_ACT_16515203
JAK2	8.85	IC50	1.4	nM	CHEMBL_ACT_18148521
JAK1	8.85	IC50	1.42	nM	CHEMBL_ACT_18737151
JAK1	8.85	IC50	1.4	nM	CHEMBL_ACT_19489501
JAK1	8.85	IC50	1.4	nM	CHEMBL_ACT_24691965
JAK1	8.85	IC50	1.42	nM	CHEMBL_ACT_27736811
JAK3	8.82	IC50	1.5	nM	CHEMBL_ACT_20638927
JAK2	8.82	IC50	1.5	nM	CHEMBL_ACT_22471583
JAK1	8.81	IC50	1.55	nM	CHEMBL_ACT_22809388
JAK1	8.8	IC50	1.6	nM	CHEMBL_ACT_12649690
JAK1	8.8	IC50	1.6	nM	CHEMBL_ACT_13282601
JAK3	8.8	IC50	1.6	nM	CHEMBL_ACT_14751947
JAK1	8.8	IC50	1.6	nM	CHEMBL_ACT_18679950
JAK1	8.8	IC50	1.6	nM	CHEMBL_ACT_19253634
JAK3	8.8	IC50	1.6	nM	CHEMBL_ACT_19433369
JAK3	8.8	IC50	1.6	nM	CHEMBL_ACT_26239379
JAK2	8.8	IC50	1.6	nM	CHEMBL_ACT_5109059
JAK1	8.8	Kd	1.6	nM	CHEMBL_ACT_7567713
JAK3	8.77	IC50	1.7	nM	CHEMBL_ACT_18957307
JAK1	8.77	IC50	1.7	nM	CHEMBL_ACT_18991869
JAK1	8.77	Kd	1.7	nM	CHEMBL_ACT_2595792
JAK2	8.74	Kd	1.8	nM	CHEMBL_ACT_2595781
JAK1	8.7	IC50	2	nM	CHEMBL_ACT_13284807
JAK3	8.7	IC50	2	nM	CHEMBL_ACT_13284841
JAK1	8.7	IC50	2	nM	CHEMBL_ACT_15082455
JAK2	8.7	IC50	2	nM	CHEMBL_ACT_18298410
JAK1	8.7	IC50	2	nM	CHEMBL_ACT_18570664
JAK3	8.68	IC50	2.1	nM	CHEMBL_ACT_18679915
JAK3	8.68	IC50	2.1	nM	CHEMBL_ACT_19253603
JAK3	8.66	IC50	2.2	nM	CHEMBL_ACT_12649732
JAK3	8.66	IC50	2.2	nM	CHEMBL_ACT_13283423
JAK1	8.66	IC50	2.2	nM	CHEMBL_ACT_24825026
JAK2	8.66	IC50	2.2	nM	CHEMBL_ACT_26230163
JAK3	8.66	IC50	2.2	nM	CHEMBL_ACT_28446002

Target pathways

Aggregated over 5 target gene(s): PKN1, JAK1, JAK2, JAK3, TYK2.

Top Reactome pathways

92 total, by targets touching each:

Pathway	Targets	Genes
Interleukin-4 and Interleukin-13 signaling	4	JAK1, JAK2, JAK3, TYK2
Interleukin-20 family signaling	4	JAK1, JAK2, JAK3, TYK2
Potential therapeutics for SARS	4	JAK1, JAK2, JAK3, TYK2
Interleukin-6 signaling	3	JAK1, JAK2, TYK2
MAPK3 (ERK1) activation	3	JAK1, JAK2, TYK2
MAPK1 (ERK2) activation	3	JAK1, JAK2, TYK2
Cytokine Signaling in Immune system	3	JAK1, JAK2, JAK3
Signal Transduction	3	JAK1, JAK2, JAK3
Disease	3	JAK1, JAK2, JAK3
Immune System	3	JAK1, JAK2, JAK3
Signaling by Interleukins	3	JAK1, JAK2, JAK3
Interleukin-2 family signaling	3	JAK1, JAK2, JAK3
Interleukin-3, Interleukin-5 and GM-CSF signaling	3	JAK1, JAK2, JAK3
Infectious disease	3	JAK1, JAK2, JAK3
RAF/MAP kinase cascade	3	JAK1, JAK2, JAK3
MAPK family signaling cascades	3	JAK1, JAK2, JAK3
MAPK1/MAPK3 signaling	3	JAK1, JAK2, JAK3
IL-6-type cytokine receptor ligand interactions	3	JAK1, JAK2, TYK2
Interleukin-35 Signalling	3	JAK1, JAK2, TYK2
Interleukin-12 signaling	3	JAK1, JAK2, TYK2
Interleukin-27 signaling	3	JAK1, JAK2, TYK2
Interleukin receptor SHC signaling	3	JAK1, JAK2, JAK3
Signaling by CSF3 (G-CSF)	3	JAK1, JAK2, TYK2
SARS-CoV Infections	3	JAK1, JAK2, JAK3
Inactivation of CSF3 (G-CSF) signaling	3	JAK1, JAK2, TYK2
Viral Infection Pathways	3	JAK1, JAK2, JAK3
Activation of STAT3 by cadherin engagement	3	JAK1, JAK2, TYK2
RAF-independent MAPK1/3 activation	2	JAK1, JAK2
Interleukin-7 signaling	2	JAK1, JAK3
Interleukin-12 family signaling	2	JAK1, JAK2
Other interleukin signaling	2	JAK1, TYK2
Interleukin-6 family signaling	2	JAK1, JAK2
Interleukin-10 signaling	2	JAK1, TYK2
Interferon gamma signaling	2	JAK1, JAK2
Regulation of IFNG signaling	2	JAK1, JAK2
Interleukin-15 signaling	2	JAK1, JAK3
Interleukin-9 signaling	2	JAK1, JAK3
Signaling by Receptor Tyrosine Kinases	2	JAK2, JAK3
Interleukin-2 signaling	2	JAK1, JAK3
Interleukin-23 signaling	2	JAK2, TYK2
Interleukin-21 signaling	2	JAK1, JAK3
Interferon alpha/beta signaling	2	JAK1, TYK2
Regulation of IFNA/IFNB signaling	2	JAK1, TYK2
Interferon Signaling	2	JAK1, JAK2
SARS-CoV-2 activates/modulates innate and adaptive immune responses	2	JAK1, TYK2
IFNG signaling activates MAPKs	2	JAK1, JAK2
Evasion by RSV of host interferon responses	2	JAK1, TYK2
Hemostasis	1	JAK2
ISG15 antiviral mechanism	1	JAK1
Antimicrobial mechanism of IFN-stimulated genes	1	JAK1

Dominant GO biological processes

GO term	Targets
protein phosphorylation	5
intracellular signal transduction	5
cell surface receptor signaling pathway via JAK-STAT	4
cytokine-mediated signaling pathway	4
cell differentiation	4
growth hormone receptor signaling pathway via JAK-STAT	4
regulation of cell-cell adhesion	4
regulation of transcription by RNA polymerase II	3
type II interferon-mediated signaling pathway	3
cellular response to virus	3
regulation of receptor signaling pathway via JAK-STAT	3
regulation of alpha-beta T cell activation	3
signal transduction	2
post-translational protein modification	2
chromatin organization	2

Indications & clinical

Indications

32 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
rheumatoid arthritis	3	MONDO:0008383	EFO:0000685
psoriatic arthritis	3	MONDO:0011849	EFO:0003778
ulcerative colitis	3	MONDO:0005101	EFO:0000729
juvenile idiopathic arthritis	3	MONDO:0011429	EFO:0002609
psoriasis	3	MONDO:0005083	EFO:0000676
ankylosing spondylitis	3	MONDO:0005306	EFO:0003898
polymyalgia rheumatica	3	MONDO:0019735	EFO:0008518
severe acute respiratory syndrome	3	MONDO:0005091	MONDO:0100096
glioblastoma	3	MONDO:0018177	EFO:0000519
Takayasu arteritis	3	MONDO:0017991	EFO:1001857
alopecia areata	2	MONDO:0005340	EFO:0004192
Crohn disease	2	MONDO:0005011	EFO:0000384
systemic sclerosis	2	MONDO:0005100	EFO:0000717
dry eye syndrome	2	MONDO:0006733	EFO:1000906
injury	2	MONDO:0021178	EFO:0000546
pneumonia	2	MONDO:0005249	EFO:0003106
nasal cavity and paranasal sinus lethal midline granuloma	2	MONDO:0006828	MONDO:0019472
Sjogren syndrome	2	MONDO:0010030	EFO:0000699
colitis	2	MONDO:0005292	EFO:0003872
pouchitis	2	MONDO:0005312	EFO:0003921
myositis disease	2	MONDO:0021167	EFO:0000783
Down syndrome	2	MONDO:0008608	EFO:0001064
cutaneous leishmaniasis	2	MONDO:0005446	EFO:0005046
myocarditis	2	MONDO:0004496	EFO:0009609
dermatomyositis	1	MONDO:0016367	EFO:0000398
chronic kidney disease	1	MONDO:0005300	EFO:0003884
kidney disorder	1	MONDO:0005240	EFO:0003086
cutaneous lupus erythematosus	1	MONDO:0005282	EFO:0003834
chronic granulomatous disease	1	MONDO:0018305	MONDO:0018305
sarcoidosis	1	MONDO:0019338	MONDO:0019338
granuloma annulare	1	MONDO:0006554	EFO:1000704
systemic lupus erythematosus	1	MONDO:0007915	MONDO:0007915

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 204.

Phase distribution

Phase	Trials
PHASE2	58
PHASE3	40
Not specified	33
PHASE4	31
PHASE1	27
PHASE1/PHASE2	6
EARLY_PHASE1	6
PHASE2/PHASE3	3

Top trials by phase / activity

NCT	Phase	Status	Title
NCT03976245	PHASE4	RECRUITING	Advanced Therapeutics in Rheumatoid Arthritis (RA)
NCT05102448	PHASE4	RECRUITING	Comparison of Tofacitinib and Methotrexate in Takayasu’s Arteritis
NCT05313620	PHASE4	RECRUITING	Effect of Tofacitinib on Coagulation and Platelet Function, and Its Role in Thromboembolic Events
NCT06095128	PHASE4	RECRUITING	A Study of Vedolizumab With Tofacitinib in Adults With Ulcerative Colitis (UC)
NCT06112665	PHASE4	RECRUITING	ToFAcitinib in Early Active Axial SpondyloarThritis:
NCT06438679	PHASE4	ENROLLING_BY_INVITATION	3T Therapy in the Treatment of MDA5-positive Dermatomyositis
NCT06465732	PHASE4	NOT_YET_RECRUITING	Efficacy and Safety of Dupilumab in Combination With Tofacitinib in Moderate to Severe Adult AD Patients
NCT06498089	PHASE4	RECRUITING	A Randomized, Controlled, Open-label, Multicenter Clinical Trial Comparing the Efficacy and Safety of a Precision Treatment Regimen Based on Clinical-molecular Phenotypes with a Conventional Treatment Regimen in the Treatment of Patients with Active Takayasu’s Arteritis
NCT06625450	PHASE4	NOT_YET_RECRUITING	TOFACITINIB vs TOFACITINIB WITH MESALAMINE IN ULCERATIVE COLITIS
NCT06945666	PHASE4	NOT_YET_RECRUITING	A Study of Iguratimod in Combination With Tofacitinib in RA Patients
NCT06998875	PHASE4	RECRUITING	A Prospective Cohort Study on Primary Cutaneous Amyloidosis
NCT07352566	PHASE4	NOT_YET_RECRUITING	Utilization of a Microdevice for Psoriasis and Atopic Dermatitis
NCT07406204	PHASE4	NOT_YET_RECRUITING	Tofacitinib vs Methotrexate for Severe Alopecia Areata (TOFA-MTX-AA)
NCT07554820	PHASE4	RECRUITING	Major Adverse Cardiovascular Events (MACE) in Rheumatoid Arthritis Patient With Moderate to Severe Disease Activity Treated With Tofacitinib and Statins vs TNF Inhibitors: TOFSTAT CLINICAL TRIAL
NCT02092467	PHASE4	COMPLETED	Safety Study Of Tofacitinib Versus Tumor Necrosis Factor (TNF) Inhibitor In Subjects With Rheumatoid Arthritis
NCT02831855	PHASE4	COMPLETED	Methotrexate Withdrawal Study of Tofacitinib Modified Release Formulation in Subjects With Rheumatoid Arthritis
NCT03281304	PHASE4	TERMINATED	A Study of Tofacitinib in Patients With Ulcerative Colitis in Stable Remission
NCT03504072	PHASE4	UNKNOWN	Risk of Tuberculous and Other Infections in Patients of Spondyloarthritis Treated With Tofacitinib in Bangladesh
NCT03800979	PHASE4	COMPLETED	Effectiveness and Safety of Tofacitinib in Patients With Extensive and Recalcitrant Alopecia Areata
NCT04299971	PHASE4	UNKNOWN	Efficiency of Methotrexate and Tofacitinib in Mild and Moderate Patients
NCT04311567	PHASE4	TERMINATED	Effects of Tofacitinib vs Methotrexate on Rheumatoid Arthritis Interstitial Lung Disease
NCT04464642	PHASE4	UNKNOWN	Tofacitinib Versus Methotrexate as the First Line DMARD in the Treatment of Rheumatoid Arthritis
NCT04485325	PHASE4	COMPLETED	Capability of Tofacitinib or Etanercept to Accelerate Tapering of NSAID and Treat-to-target Guided De-escalation of Corticosteroids in RA Patients
NCT04927000	PHASE4	UNKNOWN	The Role of Tofacitinib in Steroid Withdrawal in Rheumatoid Arthritis
NCT04928066	PHASE4	COMPLETED	The Efficacy and Safety of Tofacitinib (TF) With Iguratimod (IGU) on RA
NCT04944524	PHASE4	UNKNOWN	Comparison of Tofacitinib and Methotrexate in the Maintained Treatment of GPA
NCT05080218	PHASE4	COMPLETED	COVID-19 VaccinE Response in Rheumatology Patients
NCT05151848	PHASE4	UNKNOWN	Comparison of Adalimumab and Tofacitinib in the Treatment of Active Takayasu Arteritis
NCT05606107	PHASE4	UNKNOWN	To Compare the Efficacy and Safety of Low-dose Glucocorticoids and Tofacitinib in Alleviating Moderate to High Disease Activity Rheumatoid Arthritis for 24 Weeks
NCT06310057	PHASE4	COMPLETED	Tofacitinib in the Treatment of Refractory Axial Spondyloarthritis Patients: A Dose Escalation Study
NCT07472166	PHASE4	COMPLETED	Efficacy of Tofacitinib on Skin Thickening in Diffuse Cutaneous Systemic Sclerosis: A Comparative Study With Methotrexate
NCT03414502	PHASE3	RECRUITING	Treatment of Rheumatoid Arthritis With DMARDs: Predictors of Response
NCT04624230	PHASE3	ACTIVE_NOT_RECRUITING	Evaluation of Oral Tofacitinib in Children Aged 2 to 17 Years Old Suffering From Moderate to Severe Ulcerative Colitis
NCT04871191	PHASE3	RECRUITING	Study of Salvage Therapy to Treat Patients With Granulomatosis With Polyangiitis
NCT05326464	PHASE3	ACTIVE_NOT_RECRUITING	Tofacitinib in Recurrent GBM Patients
NCT06020144	PHASE3	ACTIVE_NOT_RECRUITING	A Phase 3 Study Comparing TLL-018 to Tofacitinib in RA Subjects With Inadequate Response or Intolerance to bDMARDs
NCT06172361	PHASE3	RECRUITING	Induction and Tapering Therapy With Tofacitinib and Glucocorticoid in Patients With Polymyalgia Rheumatica
NCT06654882	PHASE3	RECRUITING	Trial of Sequential Medications AfteR TNFi Failure in Juvenile Idiopathic Arthritis
NCT07530367	PHASE3	NOT_YET_RECRUITING	A Phase III Randomized Controlled Trial Evaluating the Efficacy and Safety of Tofacitinib Combined With Imatinib in Patients With Moderate-to-Severe Palmoplantar Pustulosis
NCT00413699	PHASE3	COMPLETED	Long-Term Effectiveness And Safety Of CP-690,550 For The Treatment Of Rheumatoid Arthritis
NCT00661661	PHASE3	COMPLETED	Long-Term, Open-Label Study Of CP-690,550 For Treatment Of Rheumatoid Arthritis In Japan
NCT00814307	PHASE3	COMPLETED	A Phase 3 Study Comparing 2 Doses of CP-690,550 vs. Placebo for Treatment of Rheumatoid Arthritis
NCT00847613	PHASE3	COMPLETED	A 2-Year Phase 3 Study Of CP-690,550 In Patients With Active Rheumatoid Arthritis On Background Methotrexate
NCT00853385	PHASE3	COMPLETED	A Phase 3 Study Comparing 2 Doses Of CP-690,550 And The Active Comparator, Humira (Adalimumab) Vs. Placebo For Treatment Of Rheumatoid Arthritis
NCT00856544	PHASE3	COMPLETED	A Study Comparing 2 Doses Of CP-690,550 Vs. Placebo For The Treatment Of Rheumatoid Arthritis In Patients On Other Background Arthritis Medications
NCT00960440	PHASE3	COMPLETED	Study of CP-690,550 Versus Placebo In Rheumatoid Arthritis Patients On Background Methotrexate With Inadequate Response To Tumor Necrosis Factor (TNF) Inhibitors
NCT01039688	PHASE3	COMPLETED	Comparing The Effectiveness And Safety Of 2 Doses Of An Experimental Drug, CP-690,550, To Methotrexate (MTX) In Patients With Rheumatoid Arthritis Who Have Not Previously Received MTX
NCT01163253	PHASE3	TERMINATED	A Long Term Study To Evaluate The Safety And Tolerability Of CP-690,550 For Patients With Moderate To Severe Chronic Plaque Psoriasis
NCT01186744	PHASE3	COMPLETED	A Study To Evaluate The Effects And Safety Of Treatment, Treatment Withdrawal, Followed By Re-Treatment With CP-690,550 In Subjects With Moderate To Severe Chronic Plaque Psoriasis
NCT01241591	PHASE3	COMPLETED	A Phase 3, Multi Site, Randomized, Double Blind, Placebo Controlled Study Of The Efficacy And Safety Comparing CP- 690,550 And Etanercept In Subjects With Moderate To Severe Chronic Plaque Psoriasis
NCT01276639	PHASE3	COMPLETED	A One-Year Study To Evaluate The Effects And Safety Of CP-690,550 In Patients With Moderate To Severe Chronic Plaque Psoriasis
NCT01309737	PHASE3	COMPLETED	A One-Year Study To Evaluate The Efficacy And Safety Of CP-690,550 For Patients With Moderate To Severe Chronic Plaque Psoriasis
NCT01458574	PHASE3	COMPLETED	A Study Of Oral CP-690,550 As A Maintenance Therapy For Ulcerative Colitis
NCT01458951	PHASE3	COMPLETED	A Study To Evaluate Both The Efficacy and Safety Profile of CP-690,550 In Patients With Moderately to Severely Active Ulcerative Colitis
NCT01465763	PHASE3	COMPLETED	A Study Evaluating The Efficacy And Safety Of CP-690,550 In Patients With Moderate To Severe Ulcerative Colitis
NCT01470612	PHASE3	COMPLETED	Long-Term Study Of CP-690,550 In Subjects With Ulcerative Colitis
NCT01500551	PHASE2/PHASE3	COMPLETED	Long-Term Safety Study Of Tofacitinib In Patients With Juvenile Idiopathic Arthritis
NCT01519089	PHASE3	COMPLETED	A Long Term Study To Evaluate The Safety, Tolerability And Efficacy Of CP-690,550 In Patients With Moderate To Severe Plaque Psoriasis And/Or Psoriatic Arthritis
NCT01815424	PHASE3	COMPLETED	A Study Evaluating The Efficacy And Safety Of CP-690,550 In Asian Subjects With Moderate To Severe Plaque Psoriasis
NCT01882439	PHASE3	COMPLETED	Tofacitinib In Psoriatic Arthritis Subjects With Inadequate Response to TNF Inhibitors
NCT01976364	PHASE3	COMPLETED	Open-Label Extension Study Of Tofacitinib In Psoriatic Arthritis
NCT02281552	PHASE3	COMPLETED	A Study To Evaluate The Safety And Efficacy Of Tofacitinib Modified Release Tablets Compared To Tofacitinib Immediate Release Tablets In Adult Patients With Rheumatoid Arthritis
NCT02566967	PHASE3	COMPLETED	An Evaluation of the Optimal Dose of Tofacitinib Needed to Achieve Low Disease Activity (LDA) or Clinical Remission in Patients With Active Rheumatoid Arthritis (RA) as Measured From a Clinical and Structural Perspective
NCT02592434	PHASE3	COMPLETED	Efficacy Study Of Tofacitinib In Pediatric JIA Population
NCT03486457	PHASE3	COMPLETED	Efficacy And Safety Of Tofacitinib In Chinese Subjects With Active Psoriatic Arthritis
NCT03502616	PHASE3	COMPLETED	Efficacy and Safety of Tofacitinib in Subjects With Active Ankylosing Spondylitis (AS)
NCT03738956	PHASE2/PHASE3	UNKNOWN	Safety and Efficacy of Tofacitinib in the Treatment of NSAID Refractory Axial Spondyloarthritis:A Clinical Trial
NCT03970837	PHASE3	TERMINATED	Efficacy and Safety of GSK3196165 Versus Placebo and Tofacitinib in Participants With Moderately to Severely Active Rheumatoid Arthritis Who Have an Inadequate Response to Conventional Synthetic (cs)/Biologic (b) Disease Modifying Anti-rheumatic Drugs (DMARDs)
NCT03980483	PHASE3	COMPLETED	Efficacy and Safety of GSK3196165 Versus Placebo and Tofacitinib in Participants With Moderately to Severely Active Rheumatoid Arthritis Who Have an Inadequate Response to Methotrexate
NCT04469114	PHASE3	COMPLETED	Tofacitinib in Hospitalized Patients With COVID-19 Pneumonia
NCT04610476	PHASE3	UNKNOWN	Impact of Tapering Immunosuppressants on Maintaining Minimal Disease Activity in Adult Subjects With Psoriatic Arthritis
NCT05749666	PHASE3	UNKNOWN	Comparison of Tofacitinib and Prednisolone in the Treatment of Active Takayasu’s Arteritis
NCT06011343	PHASE2/PHASE3	UNKNOWN	Tofacitinib Associated With Meglumine Antimoniate in Cutaneous Leishmaniasis
NCT06278402	PHASE3	COMPLETED	Efficacy of Oral Tofacitinib in Moderate to Severe Alopecia Areata, Totalis and Universalis at Tertiary Care Hospital, Karachi.
NCT04496960	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	Safety of Tofacitinib, an Oral Janus Kinase Inhibitor, in Primary Sjogren’s Syndrome
NCT05662228	PHASE2	ACTIVE_NOT_RECRUITING	Therapies for Down Syndrome Regression Disorder
NCT05845723	PHASE2	RECRUITING	Tocilizumab and Tofacitinib in the Treatment of Vascular Behçet’s Syndrome
NCT06698822	PHASE2	RECRUITING	A Phase 2 Trial to Assess Safety and Efficacy of Tofacitinib 2% Cream in the Treatment of Cutaneous T-cell Lymphoma (CTCL), Stages IA, IB, and IIA
NCT07138898	PHASE2	NOT_YET_RECRUITING	Immunosuppressant Management in Rheumatology Patients Undergoing Elective Total Shoulder Arthroplasty
NCT07281456	PHASE2	RECRUITING	Safety of Tofacitinib, an Oral Janus Kinase Inhibitor, in Primary Sjogren Disease
NCT07297069	PHASE2	NOT_YET_RECRUITING	Combination Therapy With Infliximab and Tofacitinib for Acute Severe Ulcerative Colitis - CINTO Trial
NCT07522801	PHASE2	NOT_YET_RECRUITING	A Precision Medicine Trial for Patients With Relapsed or Refractory T Cell ALL
NCT07547930	PHASE2	RECRUITING	Tofacitinib for Glucocorticoid-Resistant Moderate-to-Severe Thyroid Eye Disease
NCT07598643	PHASE2	RECRUITING	Modulation of the Immune System in Down Syndrome for Improved Outcomes and Neurodevelopment - 1
NCT00106639	PHASE2	COMPLETED	A 6-Month Study Of CP-690,550 Versus Tacrolimus In Kidney Transplant Patients
NCT00147498	PHASE2	COMPLETED	Three Dose Levels of CP-690,550 Monotherapy Versus Placebo, Administered Orally Twice Daily (BID) for 6 Weeks
NCT00263328	PHASE2	COMPLETED	Extension Study Of Stage 1 Subjects Of Study A3921009 For The Prevention Of Acute Rejection In Kidney Transplant Patient
NCT00413660	PHASE2	COMPLETED	Comparison Of 6 CP-690,550 Doses Vs.Placebo, Each Combined With Methotrexate, For The Treatment Of Rheumatoid Arthritis
NCT00483756	PHASE2	COMPLETED	Study of a JAK3 Inhibitor for the Prevention of Acute Rejection in Kidney Transplant Patients
NCT00550446	PHASE2	COMPLETED	A Phase 2 Study For Patients With A Physician’s Diagnosis Of Rheumatoid Arthritis
NCT00556257	PHASE2	WITHDRAWN	Study Of JAK3 Inhibitor For The Prevention Of Acute Rejection In Kidney Transplant Patients
NCT00603512	PHASE2	COMPLETED	Comparison Of 4 CP-690,550 Doses Vs. Placebo, Each Combined With Methotrexate, For The Treatment Of Rheumatoid Arthritis in Japan
NCT00615199	PHASE2	COMPLETED	A Study to Investigate the Safety and Efficacy of CP-690,550 in Patients With Moderate to Severe Crohn’s Disease
NCT00658359	PHASE2	COMPLETED	Extension Study Of Subjects From Study A3921030 For The Prevention Of Acute Rejection In Kidney Transplant Patients
NCT00678210	PHASE2	COMPLETED	Effectiveness and Safety of 3 Dosing Regimens of CP-690,550 to Placebo in Subjects With Moderate to Severe Chronic Plaque Psoriasis
NCT00678561	PHASE2	COMPLETED	Topical CP-690,550 For Chronic Plaque Psoriasis
NCT00687193	PHASE2	COMPLETED	Comparison Of 5 CP-690,550 Doses Vs. Placebo, For The Treatment Of Rheumatoid Arthritis In Japan
NCT00784719	PHASE1/PHASE2	COMPLETED	A Prospective, Randomized, Placebo and Active Comparator Controlled Study of CP-690,550 in Subjects With Dry Eye.
NCT00787202	PHASE2	COMPLETED	A Study To Investigate The Safety And Efficacy Of CP- 690,550 In Patients With Moderate And Severe Ulcerative Colitis.
NCT00976599	PHASE2	COMPLETED	A Study To Evaluate The Mechanism Of Action Of CP-690,550 In Patients With Rheumatoid Arthritis

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

162 molecules share ≥1 primary target. Top 100 by shared-target count:

Molecule	Source	Status	Shared targets
BARICITINIB	ChEMBL + PubChem	Phase 4 (approved)	JAK1, JAK2, JAK3, PKN1, TYK2
Crizotinib	ChEMBL + PubChem	Phase 4 (approved)	JAK1, JAK2, JAK3, PKN1, TYK2
FEDRATINIB	ChEMBL + PubChem	Phase 4 (approved)	JAK1, JAK2, JAK3, PKN1, TYK2
MIDOSTAURIN	ChEMBL + PubChem	Phase 4 (approved)	JAK1, JAK2, JAK3, PKN1, TYK2
Momelotinib	ChEMBL + PubChem	Phase 4 (approved)	JAK1, JAK2, JAK3, PKN1, TYK2
Pacritinib	ChEMBL + PubChem	Phase 4 (approved)	JAK1, JAK2, JAK3, PKN1, TYK2
Pazopanib	ChEMBL + PubChem	Phase 4 (approved)	JAK1, JAK2, JAK3, PKN1, TYK2
RUXOLITINIB	ChEMBL + PubChem	Phase 4 (approved)	JAK1, JAK2, JAK3, PKN1, TYK2
SUNITINIB	ChEMBL + PubChem	Phase 4 (approved)	JAK1, JAK2, JAK3, PKN1, TYK2
NINTEDANIB	ChEMBL	Phase 4 (approved)	JAK1, JAK2, JAK3, PKN1, TYK2
DOVITINIB	ChEMBL	Phase 3	JAK1, JAK2, JAK3, PKN1, TYK2
LESTAURTINIB	ChEMBL	Phase 3	JAK1, JAK2, JAK3, PKN1, TYK2
AT-9283	ChEMBL	Phase 2	JAK1, JAK2, JAK3, PKN1, TYK2
DECERNOTINIB	ChEMBL	Phase 2	JAK1, JAK2, JAK3, PKN1, TYK2
R-406	ChEMBL	Phase 2	JAK1, JAK2, JAK3, PKN1, TYK2
SU-014813	ChEMBL	Phase 2	JAK1, JAK2, JAK3, PKN1, TYK2
TOZASERTIB	ChEMBL	Phase 2	JAK1, JAK2, JAK3, PKN1, TYK2
Afatinib	PubChem	Approved	JAK1, JAK2, JAK3, PKN1, TYK2
Gefitinib	PubChem	Approved	JAK1, JAK2, JAK3, PKN1, TYK2
Idelalisib	PubChem	Approved	JAK1, JAK2, JAK3, PKN1, TYK2
Selumetinib	PubChem	Approved	JAK1, JAK2, JAK3, PKN1, TYK2
Axitinib	ChEMBL + PubChem	Phase 4 (approved)	JAK2, JAK3, PKN1, TYK2
BOSUTINIB	ChEMBL + PubChem	Phase 4 (approved)	JAK2, JAK3, PKN1, TYK2
Ceritinib	ChEMBL + PubChem	Phase 4 (approved)	JAK1, JAK2, JAK3, PKN1
dacomitinib	ChEMBL + PubChem	Phase 4 (approved)	JAK1, JAK3, PKN1, TYK2
DEUCRAVACITINIB	ChEMBL + PubChem	Phase 4 (approved)	JAK1, JAK2, JAK3, TYK2
Entrectinib	ChEMBL + PubChem	Phase 4 (approved)	JAK1, JAK2, JAK3, PKN1
Erlotinib	ChEMBL + PubChem	Phase 4 (approved)	JAK2, JAK3, PKN1, TYK2
Imatinib	ChEMBL + PubChem	Phase 4 (approved)	JAK1, JAK2, PKN1, TYK2
RITLECITINIB	ChEMBL + PubChem	Phase 4 (approved)	JAK1, JAK2, JAK3, TYK2
ABROCITINIB	ChEMBL	Phase 4 (approved)	JAK1, JAK2, JAK3, TYK2
DASATINIB	ChEMBL	Phase 4 (approved)	JAK2, JAK3, PKN1, TYK2
FILGOTINIB	ChEMBL	Phase 4 (approved)	JAK1, JAK2, JAK3, TYK2
PEFICITINIB	ChEMBL	Phase 4 (approved)	JAK1, JAK2, JAK3, TYK2
UPADACITINIB	ChEMBL	Phase 4 (approved)	JAK1, JAK2, JAK3, TYK2
ALVOCIDIB	ChEMBL	Phase 3	JAK2, JAK3, PKN1, TYK2
BREPOCITINIB	ChEMBL	Phase 3	JAK1, JAK2, JAK3, TYK2
DELGOCITINIB	ChEMBL	Phase 3	JAK1, JAK2, JAK3, TYK2
ITACITINIB	ChEMBL	Phase 3	JAK1, JAK2, JAK3, TYK2
ATINVICITINIB	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
AZD-1480	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
BMS-911543	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
CC-401	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
CERDULATINIB	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
GANDOTINIB	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
GOLIDOCITINIB	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
GUSACITINIB	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
IFIDANCITINIB	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
IZENCITINIB	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
NEZULCITINIB	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
NS-018	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
OCLACITINIB	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
ROPSACITINIB	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
SOLCITINIB	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
Fostamatinib	PubChem	Approved	JAK1, JAK2, PKN1, TYK2
Trametinib	PubChem	Approved	JAK1, JAK2, PKN1, TYK2
Ponatinib	ChEMBL + PubChem	Phase 4 (approved)	JAK1, JAK2, PKN1
ABIVERTINIB	ChEMBL	Phase 3	JAK1, JAK2, JAK3
DEFACTINIB	ChEMBL	Phase 3	JAK2, JAK3, TYK2
BMS-919373	ChEMBL	Phase 2	JAK2, JAK3, TYK2
CENISERTIB	ChEMBL	Phase 2	JAK2, JAK3, TYK2
LONDAMOCITINIB	ChEMBL	Phase 2	JAK1, JAK2, TYK2
SOTRASTAURIN	ChEMBL	Phase 2	JAK1, JAK3, PKN1
ZOTIRACICLIB	ChEMBL	Phase 2	JAK1, JAK2, PKN1
belumosudil	PubChem	Approved	JAK2, JAK3, TYK2
Binimetinib	PubChem	Approved	JAK1, PKN1, TYK2
regorafenib	PubChem	Approved	JAK1, PKN1, TYK2
Acalabrutinib	ChEMBL + PubChem	Phase 4 (approved)	JAK3, PKN1
Dabrafenib	ChEMBL + PubChem	Phase 4 (approved)	JAK2, PKN1
Ibrutinib	ChEMBL + PubChem	Phase 4 (approved)	JAK3, PKN1
Neratinib	ChEMBL + PubChem	Phase 4 (approved)	JAK3, PKN1
Osimertinib	ChEMBL + PubChem	Phase 4 (approved)	JAK3, PKN1
Palbociclib	ChEMBL + PubChem	Phase 4 (approved)	JAK3, PKN1
Sorafenib	ChEMBL + PubChem	Phase 4 (approved)	JAK3, PKN1
CRAVACITINIB	ChEMBL	Phase 4 (approved)	JAK2, TYK2
INFIGRATINIB	ChEMBL	Phase 4 (approved)	JAK2, TYK2
ENZASTAURIN	ChEMBL	Phase 3	JAK3, PKN1
IVARMACITINIB	ChEMBL	Phase 3	JAK1, JAK2
POVORCITINIB	ChEMBL	Phase 3	JAK1, JAK2
RUBOXISTAURIN	ChEMBL	Phase 3	JAK3, PKN1
ADAVOSERTIB	ChEMBL	Phase 2	JAK2, JAK3
FORETINIB	ChEMBL	Phase 2	JAK2, TYK2
ILORASERTIB	ChEMBL	Phase 2	JAK2, TYK2
LAUROGUADINE	ChEMBL	Phase 2	JAK2, JAK3
LEPZACITINIB	ChEMBL	Phase 2	JAK1, JAK3
PELITINIB	ChEMBL	Phase 2	JAK2, JAK3
PICTILISIB	ChEMBL	Phase 2	JAK1, TYK2
REBASTINIB	ChEMBL	Phase 2	JAK1, JAK2
SILMITASERTIB	ChEMBL	Phase 2	PKN1, TYK2
SPEBRUTINIB	ChEMBL	Phase 2	JAK2, JAK3
TG100-115	ChEMBL	Phase 2	JAK1, TYK2
CAPIVASERTIB	ChEMBL + PubChem	Phase 4 (approved)	PKN1
BRIGATINIB	ChEMBL	Phase 4 (approved)	JAK2
LORLATINIB	ChEMBL	Phase 4 (approved)	JAK2
NICLOSAMIDE	ChEMBL	Phase 4 (approved)	JAK2
PRALSETINIB	ChEMBL	Phase 4 (approved)	JAK2
REPOTRECTINIB	ChEMBL	Phase 4 (approved)	JAK2
TRIAMTERENE	ChEMBL	Phase 4 (approved)	JAK2
ZANUBRUTINIB	ChEMBL	Phase 4 (approved)	JAK3
QUERCETIN	ChEMBL + PubChem	Phase 3 (approved)	PKN1