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Xeljanz(tofacitinib)
Xeljanz (tofacitinib) is a small molecule pharmaceutical. Tofacitinib was first approved as Xeljanz on 2012-11-06. It is used to treat rheumatoid arthritis in the USA. It has been approved in Europe to treat rheumatoid arthritis. The pharmaceutical is active against tyrosine-protein kinase JAK3, tyrosine-protein kinase JAK1, and tyrosine-protein kinase JAK2. In addition, it is known to target serine/threonine-protein kinase N1 and non-receptor tyrosine-protein kinase TYK2.
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Commercial
Therapeutic Areas
Therapeutic Area
MeSH
musculoskeletal diseasesD009140
skin and connective tissue diseasesD017437
immune system diseasesD007154
Trade Name
FDA
EMA
Xeljanz (generic drugs available since 2021-08-19)
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
Tofacitinib citrate
Tradename
Company
Number
Date
Products
XELJANZCV SciencesN-203214 RX2012-11-06
2 products, RLD
XELJANZ XRMylanN-208246 RX2016-02-23
2 products, RLD
XELJANZMylanN-213082 RX2020-09-25
1 products, RLD, RS
Labels
FDA
EMA
Brand Name
Status
Last Update
xeljanzNew Drug Application2023-03-09
Indications
FDA
EMA
Indication
Ontology
MeSH
ICD-10
rheumatoid arthritisEFO_0000685D001172M06.9
Agency Specific
FDA
EMA
Expiration
Code
TOFACITINIB CITRATE, XELJANZ, PF PRISM CV
2024-12-14I-879
2023-09-25NPP
TOFACITINIB CITRATE, XELJANZ XR, PFIZER
2024-12-14I-879
TOFACITINIB CITRATE, XELJANZ, PFIZER
2023-09-25NP
Patent Expiration
Patent
Expires
Flag
FDA Information
Tofacitinib Citrate, Xeljanz Xr, Pfizer
99371812034-03-14DP
106393092034-03-14DP
112535232034-03-14U-3326, U-3327, U-3328, U-3329
Tofacitinib Citrate, Xeljanz, Pf Prism Cv
RE417832025-12-08DP
69650272023-03-25DP
ATC Codes
L: Antineoplastic and immunomodulating agents
L04: Immunosuppressants
L04A: Immunosuppressants
L04AA: Selective immunosuppressants
L04AA29: Tofacitinib
HCPCS
No data
Clinical
Clinical Trials
198 clinical trials
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Mock data
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Indications Phases 4
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Rheumatoid arthritisD001172EFO_0000685M06.971613121361
Ulcerative colitisD003093EFO_0000729K51262515
Psoriatic arthritisD015535EFO_0003778L40.51618
Alopecia areataD000506EFO_0004192L634116
Interstitial lung diseasesD017563EFO_0004244J84.89314
Takayasu arteritisD013625EFO_1001857M31.433
SpondylarthritisD02524122
Rheumatic feverD012213EFO_1001160I00-I0211
TherapeuticsD01381211
Granulomatosis with polyangiitisD014890EFO_0005297M31.311
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Indications Phases 3
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
PsoriasisD011565EFO_0000676L4026715
Covid-19D000086382U07.13115
Juvenile arthritisD001171EFO_0002609M08134
Ankylosing spondylitisD013167EFO_0003898M45112
Glycogen storage disease type iiD006009Orphanet_365E74.0211
GlioblastomaD005909EFO_000051511
Indications Phases 2
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Healthy volunteers/patients22123
Kidney transplantationD016030516
Systemic lupus erythematosusD008180EFO_0002690M32414
Crohn diseaseD003424EFO_0000384K5044
Atopic dermatitisD003876EFO_0000274L20133
Dry eye syndromesD015352H04.12122
Down syndromeD004314EFO_0001064Q9022
Polymyalgia rheumaticaD011111EFO_0008518M35.311
PouchitisD019449EFO_0003921K91.85011
Colonic pouchesD03902111
Show 18 more
Indications Phases 1
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Myasthenia gravisD009157EFO_0004991G70.011
NeoplasmsD009369C8011
AdenocarcinomaD00023011
CholangiocarcinomaD018281C22.111
Granuloma annulareD016460L92.011
SarcoidosisD012507EFO_0000690D80-D8911
Pulmonary sarcoidosisD017565DOID_13406D86.011
Discoid lupus erythematosusD008179L93.011
ColitisD003092EFO_0003872K52.911
DermatomyositisD003882EFO_0000398M3311
Show 5 more
Indications Without Phase
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Anti-neutrophil cytoplasmic antibody-associated vasculitisD056648I77.8211
Immunoglobulin g4-related diseaseD00007773311
SpondylarthropathiesD025242EFO_0000706M4711
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common nameTOFACITINIB
INNtofacitinib
Description
Tofacitinib is 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. It has a role as an EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor and an antirheumatic drug. It is a pyrrolopyrimidine, a N-acylpiperidine, a nitrile and a tertiary amino compound.
Classification
Small molecule
Drug classtyrosine kinase inhibitors: tyrosine kinase inhibitors; janus kinase inhibitors
Image (chem structure or protein)
Structure (InChI/SMILES or Protein Sequence)
C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)c1ncnc2[nH]ccc12
Identifiers
PDB3EYG
CAS-ID477600-75-2
RxCUI1357536
ChEMBL IDCHEMBL221959
ChEBI ID71200
PubChem CID9926791
DrugBankDB08895
UNII ID87LA6FU830 (ChemIDplus, GSRS)
Target
Agency Approved
JAK3
JAK3
JAK1
JAK1
JAK2
JAK2
Organism
Homo sapiens
Gene name
JAK3
Gene synonyms
NCBI Gene ID
Protein name
tyrosine-protein kinase JAK3
Protein synonyms
JAK-3, Janus kinase 3, Janus kinase 3 (a protein tyrosine kinase, leukocyte), L-JAK, Leukocyte janus kinase
Uniprot ID
Mouse ortholog
Jak3 (16453)
tyrosine-protein kinase JAK3 (Q62137)
Alternate
PKN1
PKN1
TYK2
TYK2
Organism
Homo sapiens
Gene name
PKN1
Gene synonyms
PAK1, PKN, PRK1, PRKCL1
NCBI Gene ID
Protein name
serine/threonine-protein kinase N1
Protein synonyms
PAK-1, Protease-activated kinase 1, Protein kinase C-like 1, Protein kinase C-like PKN, protein kinase C-related kinase 1, Protein kinase PKN-alpha, Protein-kinase C-related kinase 1, serine-threonine kinase N, Serine-threonine protein kinase N, serine/threonine protein kinase N
Uniprot ID
Mouse ortholog
Pkn1 (320795)
serine/threonine-protein kinase N1 (P70268)
Variants
Clinical Variant
No data
Financial
Xeljanz - Pfizer
$
£
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Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 8,830 documents
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Safety
Black-box Warning
Black-box warning for: Xeljanz
Adverse Events
Top Adverse Reactions
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71,765 adverse events reported
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