Sulfasalazine (brand name Azulfidine) is a sulfa agent and a derivative of mesalazine. Sulfasalazine inhibits in vitro growth of the human pancreatic cancer cell lines MIA PaCa-2 and PANC-1. Sulfasalazine also inhibits the cystine-glutamate antiporter, system Xc (SXC). Sulfasalazine, and its metabolite 5-ASA, are poorly absorbed from the gut. Its main mode of action is therefore believed to be inside the intestine. Sulfasalazine (Salazopyrin) induced T lymphocyte apoptosis in glioblastoma cell lines, modulated inflammatory mediators from both cyclooxygenase/5-lipoxygenase pathways and NF-κB signaling pathways, attenuated transcription of proinflammatory cytokines, and activated PPARγ. Sulfasalazine has long been used in treatment of inflammatory bowel disease, including ulcerative colitis and Crohn's disease.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 60 mg/mL|
Sulfasalazine for brain cancer fits.
Sontheimer H, et al. Expert Opin Investig Drugs. 2012 May;21(5):575-8. PMID: 22404218.
Potential use of the anti-inflammatory drug, sulfasalazine, for targeted therapy of pancreatic cancer.
Lo M, et al. Curr Oncol. 2010 Jun;17(3):9-16. PMID: 20567622.
In vitro and in vivo activity of the nuclear factor-kappaB inhibitor sulfasalazine in human glioblastomas.
Robe PA, et al. Clin Cancer Res. 2004 Aug 15;10(16):5595-603. PMID: 15328202.
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