jakinhibitors
Table of Contents
JAK inhibitors
see also:
Introduction
- the JAK-family of cytokine receptors consists of four members: JAK1, JAK2, JAK3 and TYK2 that have different association patterns to receptors and are part of the Signal Transducer and Activation of Transcription (JAK-STAT) pathway
- some JAK inhibitors are selective for specific JAK enzymes, which may influence their efficacy and safety profiles
- JAK3 inhibitors necessarily cause a loss or total absence of T cells and natural killer cells while leaving a normal amount of B cells
Potential use cases
- Rheumatoid arthritis
- Psoriatic arthritis
- Juvenile idiopathic arthritis
- Axial spondyloarthritis
- Ulcerative colitis
- Atopic dermatitis
- Alopecia areata
Potential side effects
- increased risk of infections (like shingles) - hence live vaccinations soon before starting Rx or concurrently are NOT recommended
- increased risk of major cardiovascular problems, such as heart attack and stroke, cancer, blood clots, serious infections and death, as compared with tumour necrosis factor (TNF) inhibitors1)
- elevated cholesterol
- blood clots
- hypertension
- anaemia
- headache
- diarrhoea
- increased blood creatine phosphokinase
- in some cases, increased risk of certain cancers, particularly in older adults with rheumatoid arthritis
- increases risk of acne 2.5-fold more than when atopic dermatitis patients are Rx with Th2 cytokine inhibitors
- others
General contra-indications include
- active tuberculosis and other severe infections
- recent live vaccination
- severe liver impairment (Child–Pugh score C)
- pregnancy
- most are not approved for children aged under 12 yrs
- should generally be avoided in:
- age 65 or over
- those at increased risk of cardiovascular problems such as heart attacks or stroke (eg. including current or past long-time smokers)
- those at increased risk of cancer
- those with risk factors for DVT / PE
- those who have not yet had zoster vaccination (should be done well before starting Rx)
JAK-STAT system inhibitors
pan-JAK inhibitors
- baricitinib (Olumiant)
- oral agent mainly used to Rx rheumatoid arthritis and is a disease-modifying antirheumatic drug (DMARD)
- delgocitinib (Corectim)
- treatment of atopic dermatitis
- FDA in 2025 approved topical treatment of adults with moderate to severe chronic hand eczema
JAK 1 selective inhibitors
- ivarmacitinib
- appears to be beneficial in ankylosing spondylitis (AS)
- upadacitinib (Rinvoq)
- used for the treatment of rheumatoid arthritis, psoriatic arthritis, atopic dermatitis, ulcerative colitis, Crohn's disease, ankylosing spondylitis, and axial spondyloarthritis
- tofacitinib (Xeljanz)
- JAK 1 and Jak 3 selective inhibition
- oral agent used to Rx rheumatoid arthritis, ulcerative colitis, psoriatic arthritis, ankylosing spondylitis (AS), polyarticular course juvenile idiopathic arthritis (pcJIA)
jakinhibitors.txt · Last modified: 2026/01/28 09:46 by gary1