Drug intelligence / Profile preview

upadacitinib + methotrexate + tofacitinib

Development stage
Preclinical
Lead developer
AbbVie
Modality
Small Molecules
Administration
Oral
01

Overview

A combination regimen consisting of **upadacitinib**, **methotrexate**, and **tofacitinib**. This is not a single fixed-dose combination product, but rather the concurrent or sequential use of three disease-modifying antirheumatic drugs (DMARDs) in the treatment of moderate to severe rheumatoid arthritis. All three agents individually are oral small molecule DMARDs: upadacitinib and tofacitinib are Janus kinase (JAK) inhibitors (with upadacitinib being more selective for JAK1 and tofacitinib being a pan-JAK inhibitor), and methotrexate is a folate analog metabolic inhibitor that reduces immune cell proliferation and function. This combination would be used for autoimmune disorders where robust immunosuppression is needed, though it is not a standard or approved regimen, and combination of multiple JAK inhibitors with methotrexate poses high safety risk.

Other names
upadacitinib + methotrexate + tofacitinib
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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