Drug intelligence / Profile preview

placebo + tofacitinib + methotrexate

Development stage
Unknown
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

This is a combination regimen used in clinical trials for rheumatoid arthritis, consisting of placebo, tofacitinib, and methotrexate. Tofacitinib is an oral small molecule Janus kinase (JAK) inhibitor that targets JAK1 and JAK3 (and to a lesser extent JAK2), thereby interfering with the JAK-STAT signaling pathway involved in immune cell function and inflammatory cytokine production. Methotrexate is a disease-modifying anti-rheumatic drug (DMARD) that acts as an immunosuppressant by inhibiting dihydrofolate reductase, reducing DNA synthesis and suppressing immune-mediated inflammation. Placebo serves as an inactive control in clinical studies. This combination has been studied primarily for the treatment of moderate to severe active rheumatoid arthritis in patients with inadequate response or intolerance to conventional DMARDs[1][2][6].

02

Targets

JAK3 (Janus kinase 3)JAK2 (Janus kinase 2)DHFR (Dihydrofolate reductase)JAK1 (Janus kinase 1)TYK2 (Tyrosine kinase 2)

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