Drug intelligence / Profile preview

cariporide

Development stage
Unknown
Lead developer
Hoechst
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Cariporide is a selective small molecule inhibitor of the sodium-hydrogen exchanger, primarily targeting the sodium-hydrogen exchanger isoform 1 (NHE1). It was developed to reduce myocardial injury during ischemia-reperfusion by preventing intracellular sodium and subsequent calcium overload in cardiac myocytes. By inhibiting NHE1, cariporide limits early influx of sodium ions and reduces cell death caused by oxidative stress, conferring cardioprotective effects. Although it showed promise in reducing myocardial infarction rates in clinical trials for cardiac surgery patients, its development was halted due to an observed increase in mortality associated with cerebrovascular events. Cariporide has also been investigated for potential anti-cancer properties through inhibition of NHE1 in tumor cells[1][2][3][8].

Other names
N-(diaminomethylidene)-3-(methylsulfonyl)-4-(propan-2-yl)benzamideN-(Aminoiminomethyl)-4-(1-methylethyl)-3-(methylsulfonyl)benzamideCariporide [INN]159138-80-4
02

Targets

NHE1 (Sodium/hydrogen exchanger 1)NHE2 (Sodium-hydrogen exchanger 2)NHE3 (Sodium/hydrogen exchanger 3)

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