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Enalkiren is a potent, dipeptide small molecule renin inhibitor that mimics the transition state of the human renin substrate, angiotensinogen. It acts by directly inhibiting renin, leading to suppression of plasma renin activity and reduction in angiotensin II levels. Enalkiren was developed as an antihypertensive agent and also investigated for lowering intraocular pressure in glaucoma. Clinical studies demonstrated dose-dependent reductions in blood pressure and prolonged pharmacologic activity without evidence of tachyphylaxis. Despite promising results, development for hypertension, heart failure, glaucoma, and kidney diseases was discontinued. The drug was originally developed by Abbott Laboratories.
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