Drug intelligence / Profile preview

clorexolone

Development stage
Discontinued
Lead developer
May & Baker
Modality
Small Molecules
Administration
Oral
01

Overview

Clorexolone is a sulfonamide diuretic of the phthalimidine class, chemically and pharmacologically related to chlorthalidone. Developed by May & Baker and Rhone-Poulenc in the 1960s, it functions as a thiazide-like diuretic by inhibiting the sodium-chloride symporter (NCC) in the distal convoluted tubule of the kidney. This inhibition leads to increased excretion of sodium, chloride, and water, making it effective for managing hypertension and edema associated with congestive heart failure or renal disease. Additionally, clorexolone has been studied for its potential to mitigate lithium-induced polyuria by acting on the distal nephron. Although it was marketed under brand names like Nefrolan and Flonatril, its clinical use has largely been superseded by newer antihypertensive agents.

Brand names
FlonatrilNefrolan
Other names
clorexolone5-chloro-2-cyclohexyl-1-oxo-6-sulfamoylisoindoline5-chloro-2-cyclohexyl-6-sulfamoylisoindolin-1-one
02

Targets

SLC12A3 (Thiazide-sensitive sodium-chloride cotransporter)

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