Balsalazide disodium dihydrate

Balsalazide Disodium Dihydrate (CAS No. 150399-21-6) is the dihydrated disodium salt form of Balsalazide (CAS No. 80573-04-2, Catalog No.: B3460). As a prodrug of 5-aminosalicylic acid (5-ASA), its core targets include colonic bacterial azoreductase (mediating its own cleavage and activation) and peroxisome proliferator-activated receptor γ (PPARγ, regulating anti-inflammation and cell proliferation). Its active metabolite, 5-ASA, can also inhibit cyclooxygenase (COX), lipoxygenase (LOX), and targets related to immune cell activation; its activity relies on the 5-ASA released through metabolism. The commonly used application concentration is at the microgram level (e.g., the substrate dosage in radiolabeling experiments is 100 μg, and the optimized concentration in in vitro reaction systems is combined with 75 μg of chloramine-T). In animal experiments, a low dose of 2.25 g and a medium dose of 4.5 g can be used for efficacy evaluation. The clinically effective therapeutic concentration corresponds to oral dosages: 6.75 g/day for inducing remission of mild to moderate active ulcerative colitis, the maintenance remission dose is consistent with the induction dose, and a low dose of 2.25 g can be used in combination with probiotics. Its biological activity is reflected in the local release of 5-ASA in the colon, exerting anti-inflammatory effects by inhibiting the synthesis of inflammatory mediators and blocking the proliferation of immune cells. It achieves induction of remission faster than mesalazine (average 25 days vs. 37 days) and has comparable efficacy in maintaining remission with good tolerability. Common side effects include fever, skin rash, and diarrhea; regular monitoring of renal function is required. It is indicated for the induction and maintenance of remission in mild to moderate ulcerative colitis.

References:

[1] Wiggins JB, Rajapakse R. Balsalazide: a novel 5-aminosalicylate prodrug for the treatment of active ulcerative colitis. Expert Opin Drug Metab Toxicol. 2009 Oct;5(10):1279-84. doi: 10.1517/17425250903206996. PMID: 19743890.

[2] Sanad MH, Gomaa NM, El Bakary NM, Ibrahim IT, Massoud A. Radioiodination of balsalazide, bioevaluation, and characterization as a highly selective radiotracer for imaging of ulcerative colitis in mice. J Labelled Comp Radiopharm. 2022 Mar;65(3):71-82. doi: 10.1002/jlcr.3961. Epub 2022 Jan 17. PMID: 34984721.