Tofacitinib

XELJANZ

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Pronunciation: toe-fa-SYE-ti-nib

Tofacitinib ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Tofacitinib ballicule

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

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.

Tofacitinib molecular structure (skeletal formula) — Molecular structure: Tofacitinib

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.

Available strengths

tab 5, 10 mg
sol 1 mg/mL
ER tab 11, 22 mg

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)

Cost

Tofacitinib (XELJANZ)

What pharmacies pay · NADAC 9/30/26

Strength		#/mo	generic $	brand $	CostPlus
5 mg	tab	60 BID	$34.36/mo	—	offered
10 mg	tab	60 BID	—	$6,236.31/mo	offered
1 mg/mL	sol	per unit		—	not offered

Generic entry2026

⚠ BOXED WARNINGS

Serious infections
Mortality
Malignancy
Major adverse cardiovascular events
Thrombosis

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.

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