5-Aminosalicylic Acid

5-Aminosalicylic acid (5-ASA) is a non-steroidal anti-inflammatory drug (NSAID) and an active metabolite of sulfasalazine (Item No. 15025), balsalazide (Item No. 18680), and olsalazine (Item No. 23661).¹ It is formed from these prodrugs by bacterial azoreductases in the intestinal lumen.² 5-ASA selectively inhibits COX-2 over COX-1 in isolated human whole blood (IC₅₀s = 61 and 410 µM, respectively). It inhibits hemoglobin- and hydrogen peroxide-induced lipid peroxidation in a cell-free assay (IC₅₀ = 50 µM).³ 5-ASA (100 µM) also inhibits the synthesis of leukotriene B₄ (LTB₄; Item No. 20110) in isolated human mucosal cells.⁴ Formulations containing 5-ASA have been used in the treatment of inflammatory bowel disease (IBD) and ulcerative colitis.

WARNING This product is not for human or veterinary use.

1. Warner, T.D., Giuliano, F., Vojnovic, I., et al. Nonsteroid drug selectivities for cyclo-oxygenase-1 rather than cyclo-oxygenase-2 are associated with human gastrointestinal toxicity: A full in vitro analysis. Proc. Natl. Acad. Sci. USA 96(13), 7563-7568 (1999).

2. Nugent, S.G., Kumar, D., Rampton, D.S., et al. Intestinal luminal pH in inflammatory bowel disease: Possible determinants and implications for therapy with aminosalicylates and other drugs. Gut 48(4), 571-577 (2001).

3. Beiranvand, M. A review of the biological and pharmacological activities of mesalazine or 5-aminosalicylic acid (5-ASA): An anti-ulcer and anti-oxidant drug. Inflammopharmacology 29(5), 1279-1290 (2021).

4. Schmidt, C., Fels, T., Baumeister, B., et al. The effect of 5-aminosalicylate and para-aminosalicylate on the synthesis of prostaglandin E₂ and leukotriene B₄ in isolated colonic mucosal cells. Curr. Med. Res. Opin. 13(7), 417-425 (1996).