Sevelamer (hydrochloride)

Sevelamer hydrochloride is an orally active polymeric phosphate binder and bile acid sequestrant. Sevelamer hydrochloride binds dietary phosphate in the gastrointestinal tract, reducing phosphate absorption and serum phosphorus levels, and reduces urinary phosphate excretion. Sevelamer hydrochloride binds polyanion bile acids, increases bile acid faecal excretion, and reduces total cholesterol and LDL cholesterol levels. Sevelamer hydrochloride can be used for the research of hyperphosphataemia, hyperparathyroidism, chronic renal failure, kidney disease, and type 2 diabetes^{[1][2][3][4][5][6][7][8]}. In Vitro: Sevelamer hydrochloride exhibits pH-dependent, reversible binding of AGE-BSA, with >80% binding at intestinal pH (7.0) and less than 5% binding at stomach pH (1.0), while showing minimal binding to unmodified BSA^[6].
Sevelamer (15 mg/mL; pH=6 or 8) hydrochloride decreases serum levels of gut-derived uremic toxins (such as IAA) or limits the elevation of gut-derived uremic toxins (initial concentration=1 μg/mL or 10 μg/mL)^[7]. In Vivo: Sevelamer hydrochloride produces a dose-dependent reduction in urinary phosphate excretion of up to 96% in rats with normal renal function, with greater faecal phosphate excretion than calcium carbonate^[1].
Sevelamer hydrochloride improves renal function in a rat model of long-term uraemia by reducing renal calcification^[1].
Sevelamer (1% mixed in diet; p.o.; 2-3 weeks) hydrochloride does not alter serum phosphate levels in uremic WT mice, but further decreased serum phosphate levels in uremic Npt2b / mice in uremic mouse model^[8].