Upadacitinib

Upadacitinib

  • Pregnancy category not classified yet. Animal studies showed toxic effects on fetus with skeletal & cardiovascular malformations

  • Rinvoq

  • Oral

  • JAK1

FDA

  • Rheumatoid arthritis 

Off-label

  • Atopic dermatitis (phase III trials underway)
  • Psoriasis
  • Giant cell arteritis

Boxed warning

  • Serious infections, malignancy & thrombosis 

Infections

  • Upper respiratory tract infection (most common), bacterial, fungal, viral & opportunistic

Cardiovascular

  • Thromboembolic events

Gastrointestinal

  • Perforation

Cutaneous:

  • Non-melanoma skin cancers (report of aggressive cutaneous squamous cell carcinoma),
  • Varicella zoster reactivation 

Laboratory

  • Anemia
  • Lymphopenia 
  • Neutropenia
  • Transaminitis 
  • Hyperlipidemia
  • Increase creatinine
  • Increase creatinine phosphokinase

  • Strong CYP3A4 inhibitors increase toxicity

Baseline

  • Complete blood count with differential
  • Electrolytes
  • Liver function tests
  • Lipid profile
  • Hepatitis B & C
  • Tuberculosis evaluation
  • Pregnancy test 

Follow up 

  • Annual physical exam for skin cancers 
  • Monitor for signs/symptoms of infections including tuberculosis 
  • Complete blood count with differential
  • Liver function test
  • Lipid profile
  • Repeat labs every 4-8 weeks after initiation, then every 3 months

Notes

  • Interrupt dose if hemoglobin drops <8g/dl, lymphocyte count <500 or ANC <1000
  • Avoid live vaccines