Drug intelligence / Profile preview

glucocorticoid + mesalazine

Development stage
Unknown
Lead developer
Tillotts Pharma
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Rectal, Intravenous (for Glucocorticoid Component In Hospital Settings), Topical (rectal Foam Or Enema For Distal Colitis)
01

Overview

This is a **combination therapy** of a glucocorticoid (corticosteroid) with mesalazine (also known as mesalamine or 5-aminosalicylic acid). It is used in the management of **inflammatory bowel diseases (IBD)** such as ulcerative colitis (UC) and Crohn's disease (CD). - **Glucocorticoids** are potent anti-inflammatory and immunosuppressive agents that act by binding to the glucocorticoid receptor, thereby modulating gene expression and reducing inflammatory cytokine production. They are typically used to induce remission in moderate to severe IBD, but are not suitable for long-term maintenance due to their side effect profile[3]. - **Mesalazine** is an aminosalicylate that exerts its anti-inflammatory effect primarily in the colonic mucosa by inhibiting prostaglandin and leukotriene synthesis, mainly through inhibition of prostaglandin G/H synthase (COX enzymes), and is mainly used for induction and maintenance of remission in mild to moderate ulcerative colitis[1][4]. The combination is commonly used in clinical practice, especially in moderate to severe UC, although studies indicate that adding mesalazine to corticosteroid therapy does not offer significantly greater benefit than corticosteroids alone in severe UC exacerbation[2][6]. Therapy is typically oral, but rectal administration (suppositories or enemas) may be used in distal disease. This combination targets both acute inflammation (steroids) and long-term control/prevention of relapse (mesalazine).

Other names
glucocorticoid + mesalaminecorticosteroid + mesalazinecorticosteroid + mesalaminesteroid + 5-aminosalicylic acidsteroid + 5-ASA
02

Targets

GR (Glucocorticoid receptor)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)PGHS-1 (Prostaglandin G/H Synthase 1)

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