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tofacitinib

Structure via PubChem · Public domain (PubChem)

EntityQ3530324· pop 15· linked from 377 articles

tofacitinib

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Also known as CP-690,550, CP-690550, tasocitinib, Xeljanz®

Tofacitinib, sold under the brand Xeljanz, Neojanz among others, is a medication used to treat rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, polyarticular-course juvenile idiopathic arthritis, and ulcerative colitis. It is a janus kinase (JAK) inhibitor, discovered and developed by the National Institutes of Health and Pfizer.

Chemical data

Formula
C16H20N6O
Molecular weight
312.37 g/mol
IUPAC name
3-[(3R,4R)-4-methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile
SMILES
C[C@@H]1CCN(C[C@@H]1N(C)C2=NC=NC3=C2C=CN3)C(=O)CC#N
InChIKey
UJLAWZDWDVHWOW-YPMHNXCESA-N
XLogP
1.5
Polar surface area
88.9 Ų
H-bond donors
1
H-bond acceptors
5
Formal charge
0

via PubChem

Drug data · ChEMBL

Max clinical phase
Approved
Molecule type
Small molecule
First approval
2012
Admin. routes
oral
Indications
rheumatoid arthritis, psoriatic arthritis, ulcerative colitis, alopecia areata

via ChEMBL · EBI

Wikidata facts

Mass
312.17
Show 10 more facts
chemical formula
C₁₆H₂₀N₆O
legal status (medicine)
boxed warning
isomeric SMILES
C[C@@H]1CCN(C[C@@H]1N(C)C2=NC=NC3=C2C=CN3)C(=O)CC#N
canonical SMILES
CC1CCN(CC1N(C)C2=NC=NC3=C2C=CN3)C(=O)CC#N
World Health Organisation international non-proprietary name
tofacitinib
defined daily dose
10
medical condition treated
bald head
physically interacts with
Janus kinase 3
Commons category
Tofacitinib
Sources (7)

via Wikidata · CC0

~13 min read

Encyclopedic overview

18 sections
Contents
  • Medical uses
  • Rheumatoid arthritis
  • Ulcerative colitis
  • Adverse effects
  • Mechanism
  • History
  • Society and culture
  • Economics
  • Names
  • Research
  • Psoriasis
  • Alopecia areata
  • Vitiligo
  • Atopic dermatitis
  • Ankylosing spondylitis
  • Ulcerative colitis
  • Epilepsy
  • References

{{Drugbox | Watchedfields = changed | verifiedrevid = | image = Tofacitinib.svg | image_class = skin-invert-image | width = | alt = | caption = | pronounce = | tradename = Xeljanz, Neojanz, Jaquinus, Tofacinix, Others | Drugs.com = | MedlinePlus = a613025 | DailyMedID = Tofacitinib | pregnancy_AU = D | pregnancy_AU_comment = | pregnancy_category = | routes_of_administration = By mouth | class = Janus kinase (JAK) inhibitor | ATC_prefix = L04 | ATC_suffix = AF01 | ATC_supplemental = | legal_AU = S4 | legal_AU_comment = | legal_BR = | legal_BR_comment = | legal_CA = Rx-only | legal_CA_comment = | legal_DE = | legal_DE_comment = | legal_NZ = | legal_NZ_comment = | legal_UK = POM | legal_UK_comment = | legal_US = Rx-only | legal_US_comment = | legal_EU = Rx-only | legal_EU_comment = | legal_UN = | legal_UN_comment = | legal_status = Rx-only

| bioavailability = 74% | protein_bound = 40% | metabolism = Liver (via CYP3A4 and CYP2C19) | metabolites = | onset = | elimination_half-life = 3 hours | duration_of_action = | excretion = Urine

Excerpted from Wikipedia’s “tofacitinib” article, available under the CC BY-SA 4.0 licence.