Mizagliflozin

Mizagliflozin, an orally bioavailable antidiabetic agent and a highly selective human SGLT1 (hSGLT1) inhibitor (Kᵢ ≈ 27 nM, ~303-fold selectivity over SGLT2), competitively blocks glucose absorption in the small intestine, leading to its laxative effects. This inhibition increases luminal glucose concentration, creating an osmotic gradient that promotes water retention and triggers serotonin release, ultimately stimulating peristalsis and secretion, the key components of its laxative action. Furthermore, mizagliflozin has demonstrated the ability to improve vascular cognitive impairment by preventing hippocampal neuronal death, suggestive of blood-brain barrier permeability and potential central nervous system effects.