Drug intelligence / Profile preview

benzamil

Development stage
Preclinical
Modality
Small Molecules
Administration
Topical, Inhalation, Intravenous
01

Overview

Benzamil, also known as benzyl amiloride, is a synthetic small molecule, potent analog of amiloride, and is marketed as the hydrochloride salt[1][4]. It is a selective and potent blocker of the epithelial sodium channel (ENaC), with activity several hundredfold greater than amiloride[1]. Benzamil also inhibits the sodium-calcium exchanger and certain transient receptor potential channels, such as TRPP3 and TRPA1[6]. While studied as a potential treatment for cystic fibrosis lung disease, it did not show superior efficacy to amiloride and is not clinically approved for this indication[1][3]. Recent research suggests repurposing potential for benzamil in non-small molecule indications, such as suppression of osteosarcoma cell growth and amelioration of skin inflammation, but this is preclinical[3][9]. Benzamil is primarily used as a research compound in ion transport studies[5].

Other names
Benzyl amilorideBenzamil hydrochlorideBenzamil amiloride(E)-3,5-diamino-N-(N'-benzylcarbamimidoyl)-6-chloropyrazine-2-carboxamide hydrochlorideN-(benzylamidino)-3,5-diamino-6-chloropyrazinecarboxamide hydrochlorideN-(benzylamidino)-3,5-diamino-6-chloropyrazinecarboxamide
02

Targets

DEG/ENaC/ASIC (Acid-sensing ion channel/Degenerin/Epithelial sodium channel superfamily)ENaCATP4A (Potassium–transporting ATPase alpha chain 1)SK channel (Small-conductance calcium-activated potassium channel)TRPA1 (Transient receptor potential cation channel subfamily A member 1)PKD2L1 (Polycystin-2-like 1 ion channel)NCX1 (Sodium/calcium exchanger 1)TRPC3

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