Drug intelligence / Profile preview

mesalazine + methylprednisolone + thalidomide

Development stage
Preclinical
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Rectal, Intravenous
01

Overview

This is a combination drug consisting of three active pharmaceutical ingredients: - **Mesalazine (mesalamine):** An anti-inflammatory aminosalicylate used primarily in the treatment of inflammatory bowel diseases such as ulcerative colitis. It acts locally in the colon to inhibit cyclooxygenase and lipoxygenase pathways, reducing prostaglandin and leukotriene production. - **Methylprednisolone:** A synthetic glucocorticoid corticosteroid with potent anti-inflammatory and immunosuppressive properties. It modulates gene expression to suppress pro-inflammatory cytokines and mediators. - **Thalidomide:** An immunomodulatory agent with anti-inflammatory, anti-angiogenic, and antineoplastic effects. Thalidomide inhibits tumor necrosis factor-alpha (TNF-alpha), modulates other cytokines, interferes with angiogenesis by inhibiting vascular endothelial growth factor (VEGF) pathways, and binds cereblon to induce degradation of transcription factors IKZF1/3. This combination has been studied for use in refractory ulcerative colitis where standard therapies have failed[2]. Each component targets different aspects of inflammation or immune dysregulation.

02

Targets

15-LOX (Lysyl Oxidase)CRBN (Cereblon)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)PPARG (Peroxisome proliferator-activated receptor gamma)GR (Glucocorticoid receptor)PGHS-1 (Prostaglandin G/H Synthase 1)

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