Drug intelligence / Profile preview

5-aminosalicylic acid + thiopurines

Development stage
Unknown
Modality
Small Molecules
Administration
Oral, Rectal, Intravenous
01

Overview

This is a combination therapy consisting of 5-aminosalicylic acid (also known as mesalamine or 5-ASA) and a member of the thiopurine class (such as azathioprine or 6-mercaptopurine). It is primarily used in the management of inflammatory bowel disease (IBD), including ulcerative colitis and Crohn's disease. **Mechanism of Action:** - **5-Aminosalicylic acid** acts locally in the gut to reduce inflammation by inhibiting cyclooxygenase and lipoxygenase pathways, thereby decreasing prostaglandin and leukotriene production. It also inhibits nuclear factor kappa-B kinase subunit alpha activity, reducing pro-inflammatory cytokine expression[4][7][8]. - **Thiopurines** (azathioprine, mercaptopurine) are immunosuppressive agents that act as purine antimetabolites. They are converted into active metabolites (thioguanine nucleotides) that incorporate into DNA/RNA and inhibit lymphocyte proliferation; they also induce T cell apoptosis via Rac1 inhibition[1][2][3][5][6]. The combination may have synergistic effects for inducing or maintaining remission in IBD patients who do not respond adequately to monotherapy[3].

Other names
5-ASA + thiopurinesmesalamine + thiopurinesmesalazine + thiopurines5-aminosalicylic acid plus thiopurines
02

Targets

RAC1 (Rac family small GTPase 1)PGHS-1 (Prostaglandin G/H Synthase 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)ALOX5 (Arachidonate 5-lipoxygenase)Purine salvage pathway enzymes

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