Drug intelligence / Profile preview

tofacitinib + methotrexate

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Subcutaneous, Intramuscular
01

Overview

Tofacitinib + methotrexate is a combination therapy used primarily for the treatment of moderate to severe rheumatoid arthritis, especially in patients who have had an inadequate response to methotrexate alone. Tofacitinib is an oral small molecule Janus kinase (JAK) inhibitor that targets JAK1 and JAK3, thereby blocking the JAK/STAT signaling pathway involved in immune cell function and inflammation. Methotrexate is a folate analog antimetabolite that inhibits enzymes responsible for nucleotide synthesis, such as dihydrofolate reductase, leading to suppression of inflammation and cell division. The combination has demonstrated superior efficacy compared with methotrexate monotherapy in reducing disease activity and structural progression in rheumatoid arthritis. Tofacitinib is developed and marketed by Pfizer under the brand names Xeljanz and XeljanzXR[1][2][5][6][8].

Brand names
Xeljanz
Other names
MTX
02

Targets

TYK2 (Tyrosine kinase 2)JAK2 (Janus kinase 2)DHFR (Dihydrofolate reductase)JAK1 (Janus kinase 1)ATIC (Aminoimidazole carboxamide ribonucleotide transformylase)PPAT (Amidophosphoribosyltransferase)JAK3 (Janus kinase 3)TS (Thymidylate synthase)

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