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Drug intelligence / Profile preview
tofacitinib + methotrexate
- Development stage
- Phase 4
- 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].
- Other names
- MTX
02
Targets
PPAT (Amidophosphoribosyltransferase)ATIC (Aminoimidazole carboxamide ribonucleotide transformylase)DHFR (Dihydrofolate reductase)JAK1 (Janus kinase 1)JAK2 (Janus kinase 2)JAK3 (Janus kinase 3)TYK2 (Tyrosine kinase 2)TS (Thymidylate synthase)
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