Tofacitinib Citrate is a novel Janus kinase (JAK) inhibitor used primarily for the treatment of adult patients with moderate to severe active rheumatoid arthritis (RA) who have had an inadequate response or intolerance to methotrexate.
Basic Information
English Name: Tofacitinib Citrate
CAS Number: 540737-29-9
Molecular Formula: C16H20N6O·C6H8O7
Molecular Weight: 504.50
Pharmacological Action
Tofacitinib Citrate is a JAK3/2/1 inhibitor that potently and selectively inhibits JAK3, with additional inhibition of JAK1 and JAK2. By inhibiting JAK phosphorylation, it blocks STAT phosphorylation, subsequently inhibiting the synthesis of downstream inflammatory cytokines and reducing CD4+ T cell proliferation, ultimately achieving anti-inflammatory and immunomodulatory effects.
The drug can be used in combination with methotrexate for the treatment of active rheumatoid arthritis in patients with an inadequate response to tumor necrosis factor inhibitors.
Clinical Applications
Indications: Primarily indicated for the treatment of adult patients with moderate to severe active rheumatoid arthritis (RA) who have had an inadequate response or intolerance to methotrexate.
