Tofacitinib

XELJANZ

Open Tofacitinib in the interactive console ↗

What it isJAK inhibitor; rheumatoid and psoriatic arthritis, ulcerative colitis, and ankylosing spondylitis.

Why this oneIts head-to-head safety signal against a TNF blocker moved it behind biologics and reshaped use of the entire JAK class.

What limits itSerious infection, malignancy, cardiovascular events, thrombosis, and mortality warnings drive patient selection.

FDA-approved for

rheumatoid arthritis (2012)
psoriatic arthritis, ulcerative colitis, ankylosing spondylitis

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Serious infections (incl. TB); increased mortality (RA >=50 yr with CV risk); malignancy incl. lymphoma; major adverse cardiovascular events; thrombosis.

FDA dosing	Population	Start	Target	Max
RA, PsA, or AS	Adult	5 mg BID	5 mg BID
PsA or pcJIA	Peds >=2 yr, >=10 kg	5 mg BID (>=40 kg) or weight-based (<40 kg)
Ulcerative colitis - induction	Adult	10 mg BID x8 wk (max 16 wk)		10 mg BID
Ulcerative colitis - maintenance	Adult	5 mg BID	5 mg BID	10 mg BID (shortest duration)

Renal Reduce dose in moderate or severe renal impairment (CLcr <=50 mL/min)

Hepatic Reduce dose in moderate impairment; not recommended in severe

Instructions

Do not initiate if ALC <500, ANC <1,000/mm3, or Hgb <9 g/dL.
XELJANZ XR is not substitutable with immediate-release tofacitinib.
Screen for TB and viral hepatitis before initiation.

Cautions

Serious infections (bacterial, fungal, viral, TB, opportunistic)
Increased mortality vs TNF blockers (RA >=50 yr with CV risk factor)
Malignancies incl. lymphoma and NMSC
Major adverse cardiovascular events
Thrombosis (DVT, PE, arterial)
GI perforation; lymphopenia, neutropenia, anemia, lipid elevations

Adverse reactions

Upper respiratory tract infection
Nasopharyngitis
Diarrhea
Headache
(UC) elevated cholesterol

Pregnancy Insufficient human data to assess risk

Lactation Present in human milk (published data)

⚠ BOXED WARNINGS

Serious infections
Mortality
Malignancy
Major adverse cardiovascular events
Thrombosis

Cost, est. cash$1,000–$15,000+/month

Generic entry2026

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Legacy pregnancy categoryC

Defining liabilitySerious infection, cytopenias, hepatic injury and malignancy risk require laboratory and clinical monitoring.

Mechanism of action: Tofacitinib ballicule

Tofacitinib ballicule: receptor binding, kinetics and half-life diagram

Open Tofacitinib in the interactive console ↗

Memory aids: mascots and interaction avatars

Tofacitinib XELJANZ mascot mnemonic cartoon — **“Zelly J, the Toffee City nibbler”**
jack → Janus kinase (JAK) inhibitor

Open Tofacitinib in the interactive console ↗