Drug intelligence / Profile preview

tienilic acid

Development stage
Discontinued
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

Tienilic acid is a small molecule loop diuretic with uricosuric (uric-acid lowering) action. It was formerly marketed under the brand name Selacryn for the treatment of hypertension and hyperuricaemia. Its mechanism of action involves inhibition of sodium reabsorption in the cortical diluting segment of the distal nephron in the kidney. Tienilic acid also acts as a mechanism-based inhibitor (suicide substrate) of cytochrome P450 enzyme CYP2C9. The drug was withdrawn from markets due to reports linking it to hepatotoxicity and hepatitis[1][6][7].

Brand names
Selacryn
Other names
(2,3-Dichloro-4-(2-thenoyl)phenoxy)acetic acid(2,3-Dichloro-4-(2-thiophenecarbonyl)phenoxy)acetic acid4-(2-Theonyl)-2,3-dichlorphenoxyessigsäure4-(2-Thienylketo)-2,3-dichlorophenoxyacetic acidAcide tiéniliqueácido tienilicoAcidum tienilicumThienylic acid
02

Targets

NKCC2 (Sodium-potassium-chloride cotransporter 2)CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)

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