Tofacitinib (Xeljanz)

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Mechanism of action

From the NCI Drug Dictionary: An orally available inhibitor of Janus kinases (JAK), with immunomodulatory and anti-inflammatory activities. Upon administration, tofacitinib binds to JAK and prevents the activation of the JAK-signal transducers and activators of transcription (STAT) signaling pathway. This may decrease the production of pro-inflammatory cytokines, such as interleukin (IL)-6, -7, -15, -21, interferon-alpha and -beta, and may prevent both an inflammatory response and the inflammation-induced damage caused by certain immunological diseases.

History of changes in FDA indication

Note that this drug does not have an oncology-specific label at this time.

  • 2012-11-06: Initial FDA approval for the treatment of adult patients with moderately to severely active rheumatoid arthritis who have had an inadequate response or intolerance to methotrexate. It may be used as monotherapy or in combination with methotrexate or other nonbiologic disease-modifying antirheumatic drugs (DMARDs).

Also known as

  • Code name: CP-690550
  • Generic name: tasocitinib
  • Brand name: Xeljanz