Alilusem (M17055) is under development as a novel loop diuretic for oral administration. M17055 has a potent diuretic effect and can be categorized as a loop diuretic that inhibits both the cotransport of Na+, K+, and 2Cl
- at the thick ascending Henle’s loop and the reabsorption of Na+ at the distal tubule cells in the kidney. Structure of M17055 is different from those of other loop diuretics; M17055, which has a sulfate group in its structure is soluble and well absorbed, and its bioavailability in humans is 42-60% (unpublished observation). Considering that the pKa of M17055 is 2.39, almost of M17055 would be in ionized form at physiological pH in the small intestine. In humans, the major elimination route of M17055 is renal excretion, 59-72% of the dose being recovered in unchanged form in urine; the remainder is thought to be metabolized by both CYP3A4 and CYP2C9.