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
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)
Labels
FDA
EMA
Brand Name | Status | Last Update |
|---|---|---|
| xeljanz | New Drug Application | 2023-03-09 |
Indications
FDA
EMA
Indication | Ontology | MeSH | ICD-10 |
|---|---|---|---|
| rheumatoid arthritis | EFO_0000685 | D001172 | M06.9 |
Agency Specific
FDA
EMA
Expiration | Code | ||
|---|---|---|---|
TOFACITINIB CITRATE, XELJANZ, PF PRISM CV | |||
| 2024-12-14 | I-879 | ||
| 2023-09-25 | NPP | ||
TOFACITINIB CITRATE, XELJANZ XR, PFIZER | |||
| 2024-12-14 | I-879 | ||
TOFACITINIB CITRATE, XELJANZ, PFIZER | |||
| 2023-09-25 | NP | ||
HCPCS
No data
Clinical
Clinical Trials
198 clinical trials
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Indications Phases 4
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Rheumatoid arthritis | D001172 | EFO_0000685 | M06.9 | 7 | 16 | 13 | 12 | 13 | 61 |
| Ulcerative colitis | D003093 | EFO_0000729 | K51 | — | 2 | 6 | 2 | 5 | 15 |
| Psoriatic arthritis | D015535 | EFO_0003778 | L40.5 | — | 1 | 6 | 1 | — | 8 |
| Alopecia areata | D000506 | EFO_0004192 | L63 | — | 4 | — | 1 | 1 | 6 |
| Interstitial lung diseases | D017563 | EFO_0004244 | J84.89 | — | 3 | — | 1 | — | 4 |
| Takayasu arteritis | D013625 | EFO_1001857 | M31.4 | — | — | — | 3 | — | 3 |
| Spondylarthritis | D025241 | — | — | — | 2 | — | 2 | ||
| Rheumatic fever | D012213 | EFO_1001160 | I00-I02 | — | — | — | 1 | — | 1 |
| Therapeutics | D013812 | — | — | — | 1 | — | 1 | ||
| Granulomatosis with polyangiitis | D014890 | EFO_0005297 | M31.3 | — | — | — | 1 | — | 1 |
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Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Psoriasis | D011565 | EFO_0000676 | L40 | 2 | 6 | 7 | — | — | 15 |
| Covid-19 | D000086382 | U07.1 | — | 3 | 1 | — | 1 | 5 | |
| Juvenile arthritis | D001171 | EFO_0002609 | M08 | 1 | — | 3 | — | — | 4 |
| Ankylosing spondylitis | D013167 | EFO_0003898 | M45 | — | 1 | 1 | — | — | 2 |
| Glycogen storage disease type ii | D006009 | Orphanet_365 | E74.02 | — | — | 1 | — | — | 1 |
| Glioblastoma | D005909 | EFO_0000515 | — | — | 1 | — | — | 1 |
Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Healthy volunteers/patients | — | 22 | 1 | — | — | — | 23 | ||
| Kidney transplantation | D016030 | — | 5 | — | — | 1 | 6 | ||
| Systemic lupus erythematosus | D008180 | EFO_0002690 | M32 | 4 | 1 | — | — | — | 4 |
| Crohn disease | D003424 | EFO_0000384 | K50 | — | 4 | — | — | — | 4 |
| Atopic dermatitis | D003876 | EFO_0000274 | L20 | 1 | 3 | — | — | — | 3 |
| Dry eye syndromes | D015352 | H04.12 | 1 | 2 | — | — | — | 2 | |
| Down syndrome | D004314 | EFO_0001064 | Q90 | — | 2 | — | — | — | 2 |
| Polymyalgia rheumatica | D011111 | EFO_0008518 | M35.3 | — | 1 | — | — | — | 1 |
| Pouchitis | D019449 | EFO_0003921 | K91.850 | — | 1 | — | — | — | 1 |
| Colonic pouches | D039021 | — | 1 | — | — | — | 1 |
Show 18 more
Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Myasthenia gravis | D009157 | EFO_0004991 | G70.0 | 1 | — | — | — | — | 1 |
| Neoplasms | D009369 | C80 | 1 | — | — | — | — | 1 | |
| Adenocarcinoma | D000230 | 1 | — | — | — | — | 1 | ||
| Cholangiocarcinoma | D018281 | C22.1 | 1 | — | — | — | — | 1 | |
| Granuloma annulare | D016460 | L92.0 | 1 | — | — | — | — | 1 | |
| Sarcoidosis | D012507 | EFO_0000690 | D80-D89 | 1 | — | — | — | — | 1 |
| Pulmonary sarcoidosis | D017565 | DOID_13406 | D86.0 | 1 | — | — | — | — | 1 |
| Discoid lupus erythematosus | D008179 | L93.0 | 1 | — | — | — | — | 1 | |
| Colitis | D003092 | EFO_0003872 | K52.9 | 1 | — | — | — | — | 1 |
| Dermatomyositis | D003882 | EFO_0000398 | M33 | 1 | — | — | — | — | 1 |
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 vasculitis | D056648 | I77.82 | — | — | — | — | 1 | 1 | |
| Immunoglobulin g4-related disease | D000077733 | — | — | — | — | 1 | 1 | ||
| Spondylarthropathies | D025242 | EFO_0000706 | M47 | — | — | — | — | 1 | 1 |
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | TOFACITINIB |
| INN | tofacitinib |
| 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 class | tyrosine 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
| PDB | 3EYG |
| CAS-ID | 477600-75-2 |
| RxCUI | 1357536 |
| ChEMBL ID | CHEMBL221959 |
| ChEBI ID | 71200 |
| PubChem CID | 9926791 |
| DrugBank | DB08895 |
| UNII ID | 87LA6FU830 (ChemIDplus, GSRS) |
Target
Agency Approved
JAK3
JAK3
JAK1
JAK1
JAK2
JAK2
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
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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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