Tofacitinib, the First Oral Janus Kinase Inhibitor Approved for Adult Ulcerative Colitis

J Pharm Pract. 2021 Dec;34(6):913-921. doi: 10.1177/0897190020953019. Epub 2020 Sep 2.

Abstract

Ulcerative colitis (UC) is a type of inflammatory bowel disease (IBD) characterized by chronic gastrointestinal inflammation. In most patients, the disease cycles through periods of remission and exacerbations. The complex etiology involves multiple factors including environmental, genetic, and immune causal elements. Janus Kinase (JAK) family is an essential component of a cytokine-signaling cascade partially responsible for the pathogenesis of UC. Treating UC presents difficulties despite various therapeutic options. Medications that block the JAK-signaling pathway can interfere with the inflammatory pathway of UC and possibly reduce symptoms and frequency of exacerbations. Tofacitinib is an oral pan-JAK inhibitor, primarily of JAK1 and JAK3, that was recently approved by the Food and Drug Administration (FDA) for the chronic treatment of UC in 2018. The following review describes the newly approved Janus kinase inhibitor, tofacitinib, including its pharmacokinetic properties, efficacy and safety data, and potential place in therapy.

Keywords: Janus-kinase inhibitor; Xeljanz; oral therapy; tofacitinib; ulcerative colitis.

MeSH terms

  • Adult
  • Colitis, Ulcerative* / drug therapy
  • Humans
  • Janus Kinase Inhibitors*
  • Piperidines
  • Pyrimidines
  • Pyrroles

Substances

  • Janus Kinase Inhibitors
  • Piperidines
  • Pyrimidines
  • Pyrroles
  • tofacitinib