Upadacitinib
RINVOQ
What it isJAK1-selective oral inhibitor; rheumatoid and psoriatic arthritis, atopic dermatitis, ulcerative colitis, and Crohn disease.
Why this oneIts unusually broad efficacy spans joints, skin, and both major inflammatory bowel diseases.
What limits itSerious infection, malignancy, cardiovascular events, and thrombosis are boxed; screen for tuberculosis and hepatitis B.
FDA-approved for
- rheumatoid arthritis (2019)
- atopic dermatitis, psoriatic arthritis, ulcerative colitis, Crohn disease
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Rheumatoid arthritis / ankylosing spondylitis / non-radiographic axial spondyloarthritis | Adults | 15 mg QD | 15 mg QD | 15 mg QD |
| Psoriatic arthritis | Adults | 15 mg QD | 15 mg QD | 15 mg QD |
| Psoriatic arthritis / polyarticular JIA (weight-based) | 2–<18 yr | 10–<20 kg: 3 mg BID (LQ); 20–<30 kg: 4 mg BID (LQ); ≥30 kg: 6 mg BID (LQ) or 15 mg QD tablet | per weight band | 15 mg QD (≥30 kg tablet) |
| Atopic dermatitis | ≥12 yr ≥40 kg & adults <65 yr | 15 mg QD | 15 mg QD | 30 mg QD |
| Atopic dermatitis | Adults ≥65 yr | 15 mg QD | 15 mg QD | 15 mg QD |
| Ulcerative colitis | Adults | 45 mg QD ×8 wk (induction) | 15 mg QD (maintenance) | 30 mg QD (maintenance) |
| Crohn's disease | Adults | 45 mg QD ×12 wk (induction) | 15 mg QD (maintenance) | 30 mg QD (maintenance) |
| Giant cell arteritis | Adults | 15 mg QD with tapering corticosteroids | 15 mg QD | 15 mg QD |
Renal RA/PsA/AS/nr-axSpA/pJIA/GCA: no adjustment. AD: severe (eGFR 15–<30) 15 mg QD. UC/CD: severe induction 30 mg QD, maintenance 15 mg QD. ESRD (<15): not recommended
Hepatic Mild–moderate (Child-Pugh A/B): no adjustment except UC/CD induction 30 mg QD. Severe (Child-Pugh C): not recommended
RINVOQ LQ oral solution and RINVOQ extended-release tablets are not substitutable
Instructions
- RINVOQ tablets: swallow whole, do not split/crush/chew; with or without food
- RINVOQ LQ oral solution: dosed twice daily; not substitutable with tablets
- Before starting: test/treat latent TB, screen viral hepatitis, check CBC and hepatic function, verify pregnancy status, update immunizations
- Avoid live vaccines during treatment
- Do not initiate/interrupt if ALC <500, ANC <1000, or Hgb <8 g/dL
Cautions
- Serious/opportunistic infections and TB — screen and monitor
- Viral reactivation (HBV, herpes zoster)
- Malignancy including lymphoma and NMSC
- Major adverse cardiovascular events
- Thrombosis (DVT/PE/arterial)
- Hypersensitivity (anaphylaxis, angioedema)
- GI perforation
- Hypoglycemia in patients with diabetes
- Lab abnormalities: neutropenia, lymphopenia, anemia, lipid and liver-enzyme elevations
- Embryo-fetal toxicity — use contraception
Adverse reactions
- Upper respiratory tract infection
- Herpes zoster, herpes simplex
- Bronchitis
- Nausea
- Cough
- Pyrexia
- Acne
- Headache
- Increased CPK, neutropenia
Pregnancy May cause fetal harm (animal teratogenicity); advise contraception; pregnancy surveillance program
Lactation Breastfeeding not recommended during and for 6 days after last dose
⚠ BOXED WARNINGS
- Serious infections
- Mortality
- Malignancy
- Major adverse cardiovascular events
- Thrombosis
Cost, est. cash$1,000–$15,000+/month
Generic entry2038 est.
Classes and tags
Clinical profile
Legacy pregnancy categoryNot assigned — PLLR-era drug
Defining liabilitySerious infection, cytopenias, hepatic injury and malignancy risk require laboratory and clinical monitoring.
Mechanism of action: Upadacitinib ballicule
Open Upadacitinib in the interactive console ↗
Memory aids: mascots and interaction avatars
jack → Janus kinase (JAK) inhibitor