Drug intelligence / Profile preview

methotrexate + upadacitinib

Development stage
Unknown
Lead developer
AbbVie
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Subcutaneous, Intramuscular
01

Overview

Methotrexate + upadacitinib is a combination therapy used primarily for the treatment of moderate to severe rheumatoid arthritis, particularly in patients who have had an inadequate response to conventional synthetic disease-modifying antirheumatic drugs (csDMARDs). Methotrexate is a folate antimetabolite that inhibits enzymes involved in nucleotide synthesis, leading to anti-inflammatory and immunosuppressive effects. Upadacitinib is a selective Janus kinase 1 (JAK1) inhibitor that disrupts the JAK-STAT signaling pathway, thereby reducing pro-inflammatory cytokine signaling. The combination has demonstrated greater clinical efficacy than placebo plus csDMARDs and is recommended for patients with active rheumatoid arthritis not adequately controlled by other therapies[1][2][4].

Brand names
Rinvoqmethotrexate
Other names
upadacitinib plus methotrexateupadacitinib and methotrexate
02

Targets

JAK1 (Janus kinase 1)DHFR (Dihydrofolate reductase)ATIC (Aminoimidazole carboxamide ribonucleotide transformylase)TS (Thymidylate synthase)

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