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Tofacitinib

Janus kinase (JAK1/JAK3) inhibitor · Immunosuppressant, Disease-modifying anti-rheumatic drug (DMARD)

Also known as Tofacitinib citrate, Xeljanz

START
RA/PsA 5 mg BID (or 11 mg XR daily); screen TB/hepatitis/lipids first
TYPICAL MAX
5 mg BID (RA/PsA); 10 mg BID UC induction only
STOP IF
Serious infection, MACE/thrombosis, malignancy, GI perforation, severe cytopenia
WATCH
TB/HBV screen pre-treatment, lipids 4–8 weeks, CBC/LFTs, infection/zoster, thrombosis (esp. ≥65/smokers)
CDSCO approvedSchedule HATC L04AF01
Dose laddermg/d
5start10titrate20max22ceiling
Renal dose adjustmenteGFR mL/min/1.73m²
FULLStandard dosing60REDUCEReduce to 5 mg once daily (RA/PsA)90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
11minONSET45minPEAK3h12hDURATION
ONSET
11min · absorption onset
PEAK
45min · Cmax
3h · plasma t½
DURATION
12h · BID interval
EXCRETION
Hepatic CYP3A4; ~30% renal unchanged
route + CYP
INTERACTIONS
12 major
incl. contraindicated
PREGNANCY
Avoid — embryo-fetal toxicity in animals; effective contraception during and ≥until completion
FDA category + note
Top interactionssee all 12
  • Live VaccinesContraindicatedDatabaseKimi deep-research + Cla
  • AbemaciclibSevereDatabaseDDInter
  • AcalabrutinibSevereDatabaseDDInter
  • AfliberceptSevereDatabaseDDInter
Available in India

31 branded formulations. Look up specific brands in the Drugs workspace.

Mechanism

ATP-competitive inhibition of JAK1/JAK3 (and JAK2 to a lesser extent) blocking cytokine-receptor JAK-STAT signalling (IL-2/4/7/9/15/21, interferons), modulating immune/inflammatory responses.

Indications

Rheumatoid arthritis (moderate–severe, DMARD-inadequate)Psoriatic arthritisUlcerative colitisPolyarticular juvenile idiopathic arthritis; ankylosing spondylitis

Dosing

Adult
RA/PsA: 5 mg PO twice daily or 11 mg XR once daily. Ulcerative colitis: 10 mg BID induction (8–16 weeks) then 5 mg BID maintenance.
Pediatric
pJIA ≥2 years: weight-based per label.
Renal adjustment
Moderate–severe renal impairment: 5 mg once daily (RA/PsA).
Hepatic adjustment
Moderate hepatic impairment: reduce frequency (5 mg once daily). Severe: not recommended.
Geriatric
≥65 years: higher infection/MACE/malignancy/VTE risk — use only if no alternative.
Max dose
5 mg BID (RA/PsA); 10 mg BID (UC induction only)

Pharmacokinetics

Onset
Clinical response over weeks
Peak effect
Cmax ~0.5–1 h
Duration
BID (or XR once daily)
Half-life
~3 h
Bioavailability
~74%
Protein binding
~40%
Metabolism
Hepatic CYP3A4 (CYP2C19 minor); ~30% renal unchanged
Excretion
Renal (~30% unchanged) + hepatic metabolism

Contraindications

  • Active serious infection (incl. TB)
  • Severe hepatic impairment
  • Concomitant strong immunosuppressants/biologic DMARDs
  • Hypersensitivity to tofacitinib

Side effects

Common
Upper respiratory/nasopharyngitisHeadacheDiarrhoeaRaised LDL/cholesterolRaised transaminases
Serious
  • Serious/opportunistic infections (incl. TB, herpes zoster)
  • Major adverse cardiovascular events
  • Malignancy (incl. lymphoma, lung cancer in smokers)
  • Venous and arterial thrombosis (boxed)
  • GI perforation; severe cytopenias

Pregnancy & lactation

Pregnancy

Avoid — embryo-fetal toxicity in animals; effective contraception during and ≥until completion

Lactation

Avoid breastfeeding during and for ~18 h after last dose

Drug interactions

Live Vaccines
Contraindicated
Database

Immunosuppression — disseminated infection

Update vaccines before; avoid live vaccines during

Source: Kimi deep-research + Cla

Abemaciclib
Severe
Database

Drug interaction classified as: others

Source: DDInter

Acalabrutinib
Severe
Database

Drug interaction classified as: others

Source: DDInter

Aflibercept
Severe
Database

Drug interaction classified as: others

Source: DDInter

Aldesleukin
Severe
Database

Drug interaction classified as: others

Source: DDInter

Alefacept
Severe
Database

Drug interaction classified as: others

Source: DDInter

Alemtuzumab
Severe
Database

Drug interaction classified as: others

Source: DDInter

Altretamine
Severe
Database

Drug interaction classified as: others

Source: DDInter

Amprenavir
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Anakinra
Severe
Database

Drug interaction classified as: others

Source: DDInter

Antithymocyte Immunoglobulin (rabbit)
Severe
Database

Drug interaction classified as: others

Source: DDInter

Apalutamide
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Related guidelines

Ask House about Tofacitinib

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: Goodman & Gilman 14e, Katzung, BNF·Verified: 2026-05-19 · House clinical team·Cockpit curated: 2026-05-19