Review of tofacitinib in rheumatoid arthritis

Author(s): Maria A Lopez-Olivo, Huifang Lu & Jean H Tayar

Lymphocytes play a central role in the pathogenesis of rheumatoid arthritis (RA) by releasing proinflammatory cytokines. JAK enzymes are cytoplasmic tyrosine kinases that modulate intracellular signaling transduction of the lymphocytes. JAK enzymes (JAK1, JAK2, JAK3 and TYK2) activate the signaling for gene transcription of proinflammatory cytokines, leading to joint inflammation and destruction. Tofacitinib is the first JAK inhibitor used for active RA. Its pharmacological characteristics, efficacy and safety are discussed in this review. Evidence from 11 controlled trials suggests that tofacitinib alone or combined with methotrexate is effective in patients with active disease who had failed or are intolerant to other RA therapies. Serious adverse events reported in the literature included serious infections and malignancies.