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tofacitinib + mesalamine
- Development stage
- Preclinical
- Lead developer
- Pfizer
- Modality
- Small Molecules
- Administration
- Oral, Rectal
01
Overview
The combination of tofacitinib and mesalamine is used in the treatment of ulcerative colitis (UC). This combination represents a therapeutic approach where tofacitinib, a Janus kinase (JAK) inhibitor, is administered alongside mesalamine (also known as mesalazine or 5-aminosalicylic acid/5-ASA), which is a first-line treatment for mild to moderate UC. Tofacitinib inhibits JAK1/JAK2/JAK3, preventing activation of the STAT pathway and reducing inflammatory cytokine production. Mesalamine works through topical anti-inflammatory effects on colonic epithelial cells by inhibiting cyclooxygenase, prostaglandin production, and NFkB activation. Current evidence suggests tofacitinib monotherapy may be more cost-effective than combination therapy with mesalamine in patients requiring advanced therapy for ulcerative colitis.
- Other names
- tofacitinib + 5-ASAtofacitinib + 5-aminosalicylic acid
02
Targets
JAK3 (Janus kinase 3)JAK2 (Janus kinase 2)PGHS-1 (Prostaglandin G/H Synthase 1)PPARG (Peroxisome proliferator-activated receptor gamma)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)JAK1 (Janus kinase 1)ALOX5 (Arachidonate 5-lipoxygenase)NOS2 (Nitric Oxide Synthase 2)NF-κB
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