Ipsalazide designed to release 5-aminosalicylic acid and a nontoxic carrier molecule in the gastrointestinal tract. is a novel sulfasalazine analog.
Ipsalazide is designed which the sulfapyridine of sulfasalazine has been replaced by carrier molecules.Sulfasalazine exerts beneficial effects in colitis by releasing 5-aminosalicylic acid in the colon, but its use can be limited by side effects.
No deaths or visible abnormalities occurrs within 7 days of a single oral dose of ipsalazide (4 g/kg in mice or 2 g/kg in rats). No abnormalities were seen at postmortem. The ipsalazide carrier molecule (ABG) is readily absorbed, with nearly half of the dose appearing in the urine. However, around 40% of the ABG was not recovered, and it is possible that this has undergone further metabolism, with loss of the aromatic amine function which is the basis for the colorimetric measurement of ABG.